Scientific Materials

The FDSS applications team works together with our customers to establish new applications, assays and measurement methods on our FDSS systems. Here we are able to present to you the scientific output of these fruitful collaborations.

Moreover we are happy to list user publications in well known scientific magazines.

Related Scientific Material:

Application Notes
App. Note N°. Title
FDSS Application Note N°. 1 FDSS Application Note No.1 Chloride ion sensitive fluorescent dye for Drug Screening [0.13MB/PDF]
FDSS Application Note N°. 2 FDSS Application Note No.2 CoroNa Red as a potential probe for intracellular sodium imaging [0.06MB/PDF]
FDSS Application Note N°. 3 FDSS Application Note No.3 FRET-based Voltage Sensor dyes for Drug Screening [0.06MB/PDF]
FDSS Application Note N°. 4 FDSS Application Note No.4 FDSS Cell dispensing unit for Aequorin Flash luminescence [0.5MB/PDF]
FDSS Application Note N°. 5 FDSS Application Note No.5 COX flash luminescence screening [0.06MB/PDF]
FDSS Application Note N°. 6 FDSS Application Note No.6 Direct comparison of Fast response and Slow response Membrane potential dye using the FDSS6000 [0.3MB/PDF]
FDSS Application Note N°. 7 FDSS Application Note No.7 Multiplexing Calcium Mobilization and Membrane Potential Assays Using the FDSS6000 [0.5MB/PDF]
FDSS Application Note N°. 8 FDSS Application Note No.8 Comparison of No Wash Reagent Kits on the FDSS6000 [0.4MB/PDF]
FDSS Application Note N°. 9 FDSS Application Note No.9 Effect of Plate Mixing, Fluid Addition Height and Speed on Reducing Addition Artifacts and Negative Control Drift Using the FDSS6000 [0.1MB/PDF]
FDSS Application Note N°. 10 FDSS Application Note No.10 Comparison of Orthogonal Technologies to Confirm Agonist Hits Generated Using the FDSS6000 [0.1MB/PDF]
FDSS Application Note N°. 11 FDSS Application Note No.11 Detection and Modulation of Cardiomyocyte Calcium Oscillations Using the FDSS6000 [0.1MB/PDF]
FDSS Application Note N°. 12 FDSS Application Note No.12 Fluorescence Quenching in Cell-Based Assays Can Be Dye Specific: A Case Study Using Both Fura-2 AM and Fluo-4 AM Calcium Reporter Dyes Using the FDSS6000 [0.1MB/PDF]
FDSS Application Note N°. 13 FDSS Application Note No.13 Incorporating Cell Viability Assays into High Throughput Screening Using the FDSS6000 [0.1MB/PDF]
FDSS Application Note N°. 14 FDSS Application Note No.14 Evaluation of a new intracellular calcium fluorescent reagent using the FDSS6000 [0.4MB/PDF]
FDSS Application Note N°. 15 FDSS Application Note No.15 Exposing cells to a single pulse of light of user-defined wavelength and duration using the FDSS6000 [0.1MB/PDF]
FDSS Application Note N°. 16 FDSS Application Note No.16 FluxORTM Differentially Identifies K+ Channel Antagonists Using FDSS6000 [0.1MB/PDF]
FDSS Application Note N°. 17 FDSS Application Note No.17 Use of Ca2+ oscillations in primary neuron culture: a new HTS model for neuronal diseases [0.3MB/PDF]
FDSS Application Note N°. 18 FDSS Application Note No.18 β-arrestin recruitment for GPCR Screening [0.1MB/PDF]
FDSS Application Note N°. 19 FDSS Application Note No.19 Fast kinetics enzyme assay High-throughput screening of prolyl isomerase (Pin1) inhibitors [0.2MB/PDF]
FDSS Application Note N°. 20 FDSS Application Note No.20 New Tools for Drug Discovery: Multiplexing the monitoring of Ca2+ and cAMP signaling in primary cells using the FDSS/μCell. [0.4MB/PDF]
FDSS Application Note N°. 21 FDSS Application Note No.21 Cell-based fluorescent assay for selectivity evaluation between two Na+ channels subtypes [0.2MB/PDF]
FDSS Application Note N°. 23 FDSS Application Note No.23 BRET1-assay using the FDSS/µCELL imaging plate reader [0.13MB/PDF]
FDSS Application Note N°. 24 Evaluation of membrane potential assay kit using the FDSS/μCELL imaging plate reader: Detection ion channel in nicotinic acetylcholine receptors (nAChRs) [0.1MB/PDF]
FDSS Application Note N°. 25 Identification of small molecule modulators of reactive oxygen release in TNF-α primed primary human neutrophils. [0.1MB/PDF]
FDSS Application Note N°. 26 BRET2 assay using the FDSS/µCell:
monitoring cell surface-receptor internalization
[0.1MB/PDF]
Publications

2016 | 2015 | 2014 | 2013 | 2012 | 2011 | 2010 | 2009 | 2008 | 2007 | 2006 | 2005 | 2004 | 2003 | 2002 | 2001

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2016
Authors Title Source
Stephane Bedut, Christine Seminatore-Nole, Veronique Lamamy, Sarah Caignard, Jean A. Boutin, Olivier Nosjean, Jean-Philippe Stephan, and Francis Coge High-throughput drug profiling with voltage- and calcium-sensitive fluorescent probes in human iPSC-derived cardiomyocytes American Journal of Physiology - Heart and Circulatory Physiology Published 1 July 2016 Vol. 311 no. 1, H44-H53
DOI: 10.1152/ajpheart.00793.2015
Haoyu Zeng, Maria I. Roman, Edward Lis, Armando Lagrutta, Frederick Sannajust Use of FDSS/μCell imaging platform for preclinical cardiac electrophysiology safety screening of compounds in human induced pluripotent stem cell-derived cardiomyocytes J Pharmacol Toxicol Methods. 2016 May 21.
pii: S1056-8719(16)30049-1.
doi: 10.1016/j.vascn.2016.05.009.
Kirsten Bayer Andersen, Jens Leander Johansen, Morten Hentzer, Garrick Paul Smith and Gunnar P. H. Dietz Protection of Primary Dopaminergic Midbrain Neurons by GPR139 Agonists Supports Different Mechanisms of MPP+ and Rotenone Toxicity Front. Cell. Neurosci. 10:164.
doi: 10.3389/fncel.2016.00164
Selvaraj Muthusamy, Soo Min Lee, Minghua Huang, Nam-Chul Cho, Ghilsoo Nam, Ae Nim Pae, Hyewhon Rhim, Gyochang Keum, Kyung Il Choi Isoxazoline, Isoxazole, and Oxadiazole Derivatives as M1 Muscarinic Acetylcholine Receptor Agonists Bulletin of the Korean Chemical Society. Volume 37, Issue 7, pages 1020–1028,
Version of Record online: 27 JUN 2016,
DOI: 10.1002/bkcs.10811
Olaposi I. Omotuyi, Desmond D. Adebowale, Ayodeji Famuti, Hamada Tsuyoshi Synthesis and evaluation of 6-pyrazoylamido-3N-substituted azabicyclo[3,1,0]hexane derivatives as T-type calcium channel inhibitors for treatment of neuropathic pain Bioorganic & Medicinal Chemistry. Available online 4 June 2016,
doi:10.1016/j.bmc.2016.06.006
Jung Hyun Kim, Ghilsoo Nam LPA1 extracellular loop residues 115 and 191 are not required for receptor activation but prevent Ki16425 super-antagonism RSC Advances Issue 60, 2016, Issue in Progress.
DOI: 10.1039/C6RA04276G
I. O. Omotuyi, Damilare Adebowale, Ayodeji Famuti, Tsuyoshi Hamada LPA1 Extracellular Loop residues 115 and 191 are not required for receptor activation but prevent Ki1625 super-antagonism RSC Adv., 2016, Accepted Manuscript.
DOI: 10.1039/C6RA04276G.
First published online 20 May 2016
David J. Gallacher, Gary Gintant, Najah Abiā€Gerges, Mark R. Davies, Hua Rong Lu, Kimberley M. Hoagland, Georg Rast, Brian D. Guth, Hugo M. Vargas, Robert L. Hamlin 9. Cardiac Drug Discovery Toxicology: From Target Assessment to Translational Biomarkers.
Published Online: 24 MAR 2016.
DOI: 10.1002/9781119053248.ch9
Jin-feng Yue, Guan-hua Qiao, Ni Liu, Fa-jun Nan, Zhao-bing Gao Novel KCNQ2 channel activators discovered using fluorescence-based and automated patch-clamp-based high-throughput screening techniques Acta Pharmacol Sin. 2016 Jan;37(1):105-10.
doi: 10.1038/aps.2015.142.
Dan Song, Mariko Nishiyama, Sadao Kimura Potent inhibition of angiotensin AT1 receptor signaling by RGS8: importance of the C-terminal third exon part of its RGS domain J Recept Signal Transduct Res. 2016 Oct;36(5):478-87.
doi: 10.3109/10799893.2015.1130056. Epub 2016 Jan 11.
Anja Probst Larsen, Pierre Francotte, Karla Frydenvang, Daniel Tapken, Eric Goffin, Pierre Fraikin, Daniel-Henri Caignard, Pierre Lestage, Laurence Danober, Bernard Pirotte, Jette Sandholm Kastrup Synthesis and Pharmacology of Mono-, Di-, and Trialkyl-Substituted 7-Chloro-3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-Dioxides Combined with X-ray Structure Analysis to Understand the Unexpected Structure–Activity Relationship at AMPA Receptors ACS Chem Neurosci. 2016 Mar 16;7(3):378-90.
doi: 10.1021/acschemneuro.5b00318. Epub 2016 Feb 1.
Robert A. Volkmann, Christopher M. Fanger, David R. Anderson, Venkata Ramana Sirivolu, Kathy Paschetto, Earl Gordon, Caterina Virginio, Melanie Gleyzes, Bruno Buisson, Esther Steidl, Susanna B. Mierau, Michela Fagiolini, Frank S. Menniti MPX-004 and MPX-007: New Pharmacological Tools to Study the Physiology of NMDA Receptors Containing the GluN2A Subunit PLoS One. 2016 Feb 1;11(2):e0148129.
doi: 10.1371/journal.pone.0148129. eCollection 2016.
Hiroshi Iwakura, Katsuko Dote, Mika Bando, Hiroyuki Koyama, Kiminori Hosoda, Kenji Kangawa, Kazuwa Nakao Establishment of Leptin-Responsive Cell Lines from Adult Mouse Hypothalamus PLoS One. 2016 Feb 5;11(2):e0148639.
doi: 10.1371/journal.pone.0148639. eCollection 2016.
Nicholas E. Calcaterra, Daniel J. Hoeppner, Huijun Wei, Andrew E. Jaffe, Brady J. Maher, James C. Barrow Schizophrenia-Associated hERG channel Kv11.1-3.1 Exhibits a Unique Trafficking Deficit that is Rescued Through Proteasome Inhibition for High Throughput Screening Sci Rep. 2016 Feb 16;6:19976.
doi: 10.1038/srep19976.
Noritoshi Sekido, Jun Kida, Hiroko Mashimo, Daisuke Wakamatsu, Hiroki Okada, Hidekazu Matsuya Promising Effects of a Novel EP2 and EP3 Receptor Dual Agonist, ONO-8055, on Neurogenic Underactive Bladder in a Rat Lumbar Canal Stenosis Model J Urol. 2016 Feb 13. pii: S0022-5347(16)00321-9.
doi: 10.1016/j.juro.2016.02.064. [Epub ahead of print]
Matthew Volgraf, Benjamin D. Sellers, Yu Jiang, Guosheng Wu, Cuong Q. Ly, Elisia Villemure, Richard M. Pastor, Po-wai Yuen, Aijun Lu, Xifeng Luo, Mingcui Liu, Shun Zhang, Liang Sun, Yuhong Fu, Patrick J. Lupardus, Heidi J.A. Wallweber, Bianca M. Liederer, Gauri Deshmukh, Emile Plise, Suzanne Tay, Paul Reynen, James Herrington, Amy Gustafson, Yichin Liu, Akim Dirksen, Matthias G. A. Dietz, Yanzhou Liu, Tzu-Ming Wang, Jesse E. Hanson, David Hackos, Kimberly Scearce-Levie, Jacob B. Schwarz Discovery of GluN2A-Selective NMDA Receptor Positive Allosteric Modulators (PAMs): Tuning Deactivation Kinetics via Structure-Based Design J Med Chem. 2016 Mar 24;59(6):2760-79.
doi: 10.1021/acs.jmedchem.5b02010. Epub 2016 Mar 8.
Juan C. del Álamo, Derek Lemons, Ricardo Serrano, Alex Savchenko, Fabio Cerignoli, Rolf Bodmer, Mark Mercola High throughput physiological screening of iPSC-derived cardiomyocytes for drug development Biochim Biophys Acta. 2016 Mar 4.
pii: S0167-4889(16)30047-7.
doi: 10.1016/j.bbamcr.2016.03.003. [Epub ahead of print]
Qing Zhang, Hui Yang, Jing Li, Xin Xie Discovery and Characterization of a Novel Small-Molecule Agonist for Medium-Chain Free Fatty Acid Receptor G Protein–Coupled Receptor 84 J Pharmacol Exp Ther. 2016 May;357(2):337-44.
doi: 10.1124/jpet.116.232033. Epub 2016 Mar 9.
Koteswara Rao Valasani, Qinru Sun, Du Fang, Zhihua Zhang, Qing Yu, Yaopeng Guo, Jianping Li, Anuradha Roy, Shirley ShiDu Yan Identification of a Small Molecule Cyclophilin D Inhibitor for Rescuing Aβ-Mediated Mitochondrial Dysfunction ACS Med Chem Lett. 2016 Jan 6;7(3):294-9.
doi: 10.1021/acsmedchemlett.5b00451.
eCollection 2016.
Masaomi Terajima, Yoko Kaneko-Kobayashi, Naoto Nakamura, Masatoshi Yuri, Masashi Hiramoto, Masanori Naitou, Kazuyuki Hattori, Hiroyuki Yokota, Hidekazu Mizuhara, Yasuyuki Higashi Inhibition of c-Rel DNA binding is critical for the anti-inflammatory effects of novel PIKfyve inhibitor Eur J Pharmacol. 2016 Jun 5;780:93-105.
doi: 10.1016/j.ejphar.2016.03.036.
Epub 2016 Mar 19.
Kazumi Koga, Mitsukane Yoshinaga, Yoshikatsu Uematsu, Yuji Nagai, Naoki Miyakoshi, Yoko Shimoda, Masayuki Fujinaga, Takafumi Minamimoto, Ming-Rong Zhang, Makoto Higuchi, Norikazu Ohtake, Tetsuya Suhara, Shigeyuki Chaki TASP0434299: A Novel Pyridopyrimidin-4-One Derivative as a Radioligand for Vasopressin V1B Receptor J Pharmacol Exp Ther. 2016 Jun;357(3):495-508.
doi: 10.1124/jpet.116.232942.
Epub 2016 Mar 30.
Bingqing Xia, Sui Fang, Xueqin Chen, Hong Hu, Peiyuan Chen, Huayi Wang, Zhaobing Gao MLKL forms cation channels Cell Res. 2016 May;26(5):517-28.
doi: 10.1038/cr.2016.26.
Epub 2016 Apr 1.
Arturo Picones, Arlet Loza-Huerta, Pedro Segura-Chama, Cesar O. Lara-Figueroa Chapter Nine – Contribution of Automated Technologies to Ion Channel Drug Discovery Adv Protein Chem Struct Biol. 2016;104:357-78.
doi: 10.1016/bs.apcsb.2016.01.002.
Epub 2016 Mar 3.
Wenkang Huang, Qiancheng Shen, Xubo Su, Mingfei Ji, Xinyi Liu, Yingyi Chen, Shaoyong Lu, Hanyi Zhuang, Jian Zhang BitterX: a tool for understanding bitter taste in humans Sci Rep. 2016 Apr 4;6:23450.
doi: 10.1038/srep23450.
Zhenwei Su, Emily C. Brown, Weiwei Wang, Roderick MacKinnon Novel cell-free high-throughput screening method for pharmacological tools targeting K+ channels Proc Natl Acad Sci U S A. 2016 May 17;113(20):5748-53.
doi: 10.1073/pnas.1602815113.
Epub 2016 Apr 18.
Aleksandra Klimas, Christina M. Ambrosi, Jinzhu Yu, John C. Williams, Harold Bien, Emilia Entcheva OptoDyCE as an automated system for high-throughput all-optical dynamic cardiac electrophysiology Nat Commun. 2016 May 10;7:11542.
doi: 10.1038/ncomms11542.
Daniel R. Swale, Haruto Kurata, Sujay V. Kharade, Jonathan Sheehan, Rene Raphemot, Karl R. Voigtritter Eric E. Figueroa, Jens Meiler, Anna L. Blobaum, Craig W. Lindsley, Corey R. Hopkins, Jerod S. Denton ML418: The First Selective, Sub-Micromolar Pore Blocker of Kir7.1 Potassium Channels ACS Chem Neurosci. 2016 May 24.
[Epub ahead of print]
Takuya Nagashima, Hisashi Shirakawa, Takayuki Nakagawa, Shuji Kaneko Prevention of antipsychotic-induced hyperglycaemia by vitamin D: a data mining prediction followed by experimental exploration of the molecular mechanism Sci Rep. 2016 May 20;6:26375.
doi: 10.1038/srep26375.
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2015
Authors Title Source
Olaposi I. Omotuyi, Jun Nagai & Hiroshi Ueda Lys39-Lysophosphatidate Carbonyl Oxygen Interaction Locks LPA1 N-terminal Cap to the Orthosteric Site and partners Arg124 During Receptor Activation Scientific Reports 5, Article number: 13343(2015)
doi:10.1038/srep13343
Robert L. Bertekap Jr., Neil T. Burford, Zhuyin Li, Andrew Alt High-Throughput Screening for Allosteric Modulators of GPCRs G Protein-Coupled Receptors in Drug Discovery. Volume 1335 of the series Methods in Molecular Biology
pp 223-240
Minjoo Kim, Youngjae Kim, Seon Hee Seo, Du-Jong Baek, Sun-Joon Min, Gyochang Keum, Hyunah Choo Synthesis and Biological Evaluation of N 3-Alkyl-Thienopyrimidin-4-Ones as mGluR1 Antagonists Bulletin of the Korean Chemical Society. Volume 36, Issue 5, pages 1439–1451,
Version of Record online: 28 APR 2015,
DOI: 10.1002/bkcs.10283
Huailing Zhong, Xinyan Huang, Dario Doller Multiplexing Label-Free and Fluorescence-Based Methods for Pharmacological Characterization of GPCR Ligands Label-Free Biosensor Methods in Drug Discovery. Part of the series Methods in Pharmacology and Toxicology
pp 215-231
Hilde Lavreysen, John Atack Receptors: Functional Assays Encyclopedia of Psychopharmacology.
pp 1447-1456
Elizabeth A. Ennis, Jane Wright, Cassandra L. Retzlaff, Owen B. McManus, Zhinong Lin, Xiaofang Huang, Meng Wu, Min Li, J. Scott Daniels, Craig W. Lindsley, Corey R. Hopkins, Randy D. Blakely Identification and Characterization of ML352: A Novel, Noncompetitive Inhibitor of the Presynaptic Choline Transporter ACS Chem Neurosci. 2015 Mar 18;6(3):417-27.
doi: 10.1021/cn5001809.
Epub 2015 Feb 2.
Masoud Ghamari-Langroudi, Gregory J. Digby, Julien A. Sebag, Glenn L. Millhauser, Rafael Palomino, Robert Matthews, Taneisha Gillyard, Brandon L. Panaro, Iain R. Tough, Helen M. Cox, Jerod S. Denton, Roger D. Cone G-protein-independent coupling of MC4R to Kir7.1 in hypothalamic neurons Nature. 2015 Apr 2;520(7545):94-8
doi: 10.1038/nature14051.
Epub 2015 Jan 19.
Jennie L. Conroy, R. Benjamin Free, David R. Sibley Identification of G Protein-Biased Agonists That Fail To Recruit β-Arrestin or Promote Internalization of the D1 Dopamine Receptor ACS Chem Neurosci. 2015 Apr 15;6(4):681-92.
doi: 10.1021/acschemneuro.5b00020.
Epub 2015 Feb 20.
Lothar Lindemann, Richard H. Porter, Sebastian H. Scharf, Basil Kuennecke, Andreas Bruns, Markus von Kienlin, Anthony C. Harrison, Axel Paehler, Christoph Funk, Andreas Gloge, Manfred Schneider, Neil J. Parrott, Liudmila Polonchuk, Urs Niederhauser, Stephen R. Morairty, Thomas S. Kilduff, Eric Vieira, Sabine Kolczewski, Juergen Wichmann, Thomas Hartung, Michael Honer, Edilio Borroni, Jean-Luc Moreau, Eric Prinssen, Will Spooren, Joseph G. Wettstein, Georg Jaeschke Pharmacology of Basimglurant (RO4917523, RG7090), a Unique Metabotropic Glutamate Receptor 5 Negative Allosteric Modulator in Clinical Development for Depression J Pharmacol Exp Ther. 2015 Apr;353(1):213-33.
doi: 10.1124/jpet.114.222463.
Epub 2015 Feb 9.
Lothar Lindemann, Richard H Porter, Sebastian H Scharf, Basil Kuennecke, Andreas Bruns, Markus von Kienlin, Anthony C Harrison, Axel Paehler, Christoph Funk, Andreas Gloge, Manfred Schneider, Neil J Parrott, Liudmila Polonchuk, Urs Niederhauser, Stephen R Pharmacology of basimglurant (RO4917523, RG7090), a unique mGlu5 negative allosteric modulator in clinical development for depression J Pharmacol Exp Ther. 2015 Apr;353(1):213-33.
doi: 10.1124/jpet.114.222463.
Epub 2015 Feb 9.
Gyeong hi Cho, TaeHun Kim, Woo Seung Son, Seon Hee Seo, Sun-Joon Min, Yong Seo Cho, Gyochang Keum, Kyu-Sung Jeong, Hun Yeong Koh, Jiyoun Lee, Ae Nim Pae Synthesis and biological evaluation of aryl isoxazole derivatives as metabotropic glutamate receptor 1 antagonists: A potential treatment for neuropathic pain Bioorg Med Chem Lett. 2015 Mar 15;25(6):1324-8.
doi: 10.1016/j.bmcl.2015.01.035.
Epub 2015 Jan 24.
Ryo Suzuki, Dai Nozawa, Aya Futamura, Rie Nishikawa-Shimono, Masahito Abe, Nobutaka Hattori, Hiroshi Ohta, Yuko Araki, Daiji Kambe, Mari Ohmichi, Seiken Tokura, Takeshi Aoki, Norikazu Ohtake, Hiroshi Kawamoto Discovery and in vitro and in vivo profiles of N-ethyl-N-[2-[3-(5-fluoro-2-pyridinyl)-1H-pyrazol-1-yl]ethyl]-2-(2H-1,2,3-triazol-2-yl)-benzamide as a novel class of dual orexin receptor antagonist Bioorg Med Chem. 2015 Mar 15;23(6):1260-75.
doi: 10.1016/j.bmc.2015.01.044.
Epub 2015 Feb 10.
Yasuo Yonetomi, Tomohiko Sekioka, Michiaki Kadode, Tetsuya Kitamine, Akihiro Kamiya, Naoya Matsumura, Manabu Fujita, Kazuhito Kawabata Leukotriene C4 induces bronchoconstriction and airway vascular hyperpermeability via the cysteinyl leukotriene receptor 2 in S-hexyl glutathione-treated guinea pigs Eur J Pharmacol. 2015 May 5;754:98-104.
doi: 10.1016/j.ejphar.2015.02.014.
Epub 2015 Feb 20.
Hamid R. Hoveyda, Graeme L. Fraser, Marie-Odile Roy, Guillaume Dutheuil, Frédéric Batt, Mohamed El Bousmaqui, Julien Korac, François Lenoir, Alexey Lapin, Sophie Noël, Sébastien Blanc Discovery and Optimization of Novel Antagonists to the Human Neurokinin-3 Receptor for the Treatment of Sex-Hormone Disorders (Part I) J Med Chem. 2015 Apr 9;58(7):3060-82.
doi: 10.1021/jm5017413.
Epub 2015 Mar 18.
Hamid R. Hoveyda, Graeme L. Fraser, Marie-Odile Roy, Guillaume Dutheuil, Frédéric Batt, Mohamed El Bousmaqui, Julien Korac, François Lenoir, Alexey Lapin, Sophie Noël, Sébastien Blanc Discovery and Optimization of Novel Antagonists to the Human Neurokinin-3 Receptor for the Treatment of Sex-Hormone Disorders (Part I) J Med Chem. 2015 Apr 9;58(7):3060-82.
doi: 10.1021/jm5017413.
Epub 2015 Mar 18.
Haibo Yu, Beiyan Zou, Xiaoliang Wang, Min Li Effect of tyrphostin AG879 on Kv4.2 and Kv4.3 potassium channels Br J Pharmacol. 2015 Jul;172(13):3370-82.
doi: 10.1111/bph.13127.
Epub 2015 Apr 24.
Haibo Yu, Beiyan Zou, Xiaoliang Wang, Min Li Effect of tyrphostin AG879 on Kv4.2 and Kv4.3 potassium channels Br J Pharmacol. 2015 Jul;172(13):3370-82.
doi: 10.1111/bph.13127.
Epub 2015 Apr 24.
Ni Ai, Richard D. Wood, William J. Welsh Identification of Nitazoxanide as a Group I Metabotropic Glutamate Receptor Negative Modulator for the Treatment of Neuropathic Pain: An In Silico Drug Repositioning Study Pharm Res. 2015 Aug;32(8):2798-807.
doi: 10.1007/s11095-015-1665-7.
Epub 2015 Mar 12.
Minghua Huang, Dae-Hwan Suk, Nam-Chul Cho, Deepak Bhattarai, Soon Bang Kang, Youseung Kim, Ae Nim Pae, Hyewhon Rhim, Gyochang Keum Synthesis and biological evaluation of isoxazoline derivatives as potent M1 muscarinic acetylcholine receptor agonists Bioorg Med Chem Lett. 2015 Apr 1;25(7):1546-51.
doi: 10.1016/j.bmcl.2015.02.012.
Epub 2015 Feb 16.
Shinsaku Yamane, Tomohiro Karakawa, Satoshi Nakayama, Kazufumi Nagai, Kazumi Moriyuki, Shinichi Neki, Fumitaka Suto, Tohru Kambe, Yasushi Hirota, Kazuhito Kawabata IOP-Lowering Effect of ONO-9054, A Novel Dual Agonist of Prostanoid EP3 and FP Receptors, in Monkeys Invest Ophthalmol Vis Sci.
2015 Apr;56(4):2547-52.
doi: 10.1167/iovs.14-16181.
Satoshi Itadani, Shinya Takahashi, Masaki Ima, Tetsuya Sekiguchi, Yoshiyuki Aratani, Hiromu Egashir, Naoya Matsumura, Atsuto Inoue, Yasuo Yonetomi, Manabu Fujita, Yoshisuke Nakayama, Jun Takeuchi Discovery of a potent, orally available dual CysLT1 and CysLT2 antagonist with dicarboxylic acid Bioorg Med Chem. 2015 May 1;23(9):2079-97.
doi: 10.1016/j.bmc.2015.03.011.
Epub 2015 Mar 7.
Youngjae Kim, Minjoo Kim, Mooseong Park, Jinsung Tae, Du-Jong Baek, Ki Duk Park, Hyunah Choo Synthesis of Novel Dihydropyridothienopyrimidin-4,9-dione Derivatives Molecules. 2015 Mar 19;20(3):5074-84.
doi: 10.3390/molecules20035074.
Taro Kato, Makoto Takata, Maiko Kitaichi, Momoe Kassai, Mitsuhiro Inoue, Chihiro Ishikawa, Wataru Hirose, Kozo Yoshida, Isao Shimizu DSR-98776, a novel selective mGlu5 receptor negative allosteric modulator with potent antidepressant and antimanic activity Eur J Pharmacol. 2015 Jun 15;757:11-20.
doi: 10.1016/j.ejphar.2015.03.024.
Epub 2015 Mar 28.
William H. Parsons, Raul R. Calvo, Wing Cheung, Yu-Kai Lee, Sharmila Patel, Jian Liu, Mark A. Youngman, Scott L. Dax, Dennis Stone, Ning Qin, Tasha Hutchinson, Mary Lou Lubin, Sui-Po Zhang, Michael Finley, Yi Liu, Michael R. Brandt, Christopher M. Flores, Mark R. Player Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep) J Med Chem. 2015 May 14;58(9):3859-74.
doi: 10.1021/acs.jmedchem.5b00132.
Epub 2015 Apr 15.
Yu Du, Emily Days, Ian Romaine, Kris K. Abney, Kristian Kaufmann, Gary Sulikowski, Shaun Stauffer, Craig W. Lindsley, C. David Weaver Development and Validation of a Thallium Flux-Based Functional Assay for the Sodium Channel NaV1.7 and Its Utility for Lead Discovery and Compound Profiling ACS Chem Neurosci. 2015 Jun 17;6(6):871-8.
doi: 10.1021/acschemneuro.5b00004.
Epub 2015 Apr 30.
Andrew V. Dix, Jennie L. Conroy, Kara M. George Rosenker, David R. Sibley, Daniel H. Appella PNA-Based Multivalent Scaffolds Activate the Dopamine D2 Receptor ACS Med Chem Lett. 2015 Mar 13;6(4):425-9.
doi: 10.1021/ml500478m.
eCollection 2015.
S.-H. Choi, M.-K. Hong, H.-J. Kim, N. Ryoo, H. Rhim, S.-Y. Nah, L.-W. Kang Structure of ginseng major latex-like protein 151 and its proposed lysophosphatidic acid-binding mechanism Acta Crystallogr D Biol Crystallogr. 2015 May;71(Pt 5):1039-50.
doi: 10.1107/S139900471500259X.
Epub 2015 Apr 24.
Yu Yoshida, Yoshimitsu Naoe, Taro Terauchi, Fumihiro Ozaki, Takashi Doko, Ayumi Takemura, Toshiaki Tanaka, Keiichi Sorimachi, Carsten T. Beuckmann, Michiyuki Suzuki, Takashi Ueno, Shunsuke Ozaki, Masahiro Yonaga Discovery of (1R,2S)-2-{[(2,4-Dimethylpyrimidin-5-yl)oxy]methyl}-2-(3-fluorophenyl)-N-(5-fluoropyridin-2-yl)cyclopropanecarboxamide (E2006): A Potent and Efficacious Oral Orexin Receptor Antagonist J Med Chem. 2015 Jun 11;58(11):4648-64.
doi: 10.1021/acs.jmedchem.5b00217.
Epub 2015 May 22.
Mina Nam, TaeHun Kim, Jinsook Kwak, d, Seon Hee Seo, Min Kyung Ko, Eun Jeong Lim, Sun-Joon Min, Yong Seo Cho, Gyochang Keum, Du-Jong Baek, Jiyoun Lee, Ae Nim Pae Discovery and biological evaluation of tetrahydrothieno[2,3-c]pyridine derivatives as selective metabotropic glutamate receptor 1 antagonists for the potential treatment of neuropathic pain Eur J Med Chem. 2015 Jun 5;97:245-58.
doi: 10.1016/j.ejmech.2015.04.060.
Epub 2015 Apr 30.
Shigeyuki Chaki, Toshiharu Shimazaki, Mariko Nishiguchi, Takeo Funakoshi, Michihiko Iijima, Akie Ito, Kosuke Kanuma, Yoshinori Sekiguchi Antidepressant/anxiolytic potential and adverse effect liabilities of melanin-concentrating hormone receptor 1 antagonists in animal models Pharmacol Biochem Behav. 2015 Aug;135:154-68.
doi: 10.1016/j.pbb.2015.05.018.
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Cheryl Carson, Pichai Raman, Jennifer Tullai, Lei Xu, Martin Henault, Emily Thomas, Sarita Yeola, Jianmin Lao, Mark McPate, J. Martin Verkuyl, George Marsh, Jason Sarber, Adam Amaral, Scott Bailey, Danuta Lubicka, Helen Pham, Nicolette Miranda, Jian Ding, Hai-Ming Tang, Haisong Ju, Pamela Tranter, Nan Ji, Philipp Krastel, Rishi K. Jain, Andrew M. Schumacher, Joseph J. Loureiro, Elizabeth George, Giuliano Berellini, Nathan T. Ross, Simon M. Bushell, Gül Erdemli, Jonathan M. Solomon Englerin A Agonizes the TRPC4/C5 Cation Channels to Inhibit Tumor Cell Line Proliferation PLoS One. 2015 Jun 22;10(6):e0127498.
doi: 10.1371/journal.pone.0127498.
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Yasuhiro Wada, Hiromitsu Shirahashi, Taisuke Iwanami, Masami Ogawa, Seiji Nakano, Akifumi Morimoto, Ken-ichi Kasahara, Eiichi Tanaka, Yoshio Takada, Shigeki Ohashi, Mutsuhiro Mori, Satoshi Shuto Discovery of Novel Indazole Derivatives as Highly Potent and Selective Human β3-Adrenergic Receptor Agonists with the Possibility of Having No Cardiovascular Side Effects J Med Chem. 2015 Aug 13;58(15):6048-57.
doi: 10.1021/acs.jmedchem.5b00638.
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Icilio Cavero, Henry Holzgrefe CiPA: Ongoing testing, future qualification procedures, and pending issues J Pharmacol Toxicol Methods. 2015 Nov-Dec;76:27-37.
doi: 10.1016/j.vascn.2015.06.004.
Epub 2015 Jul 6.
Satoshi Itadani, Kentaro Yashiro, Yoshiyuki Aratani, Tetsuya Sekiguchi, Atsushi Kinoshita, Hideki Moriguchi, Nobukazu Ohta, Shinya Takahashi, Akiharu Ishida, Yohei Tajima, Katsuya Hisaichi, Masaki Ima, Junya Ueda, Hiromu Egashira, Tomohiko Sekioka, Michiaki Kadode, Yasuo Yonetomi, Takafumi Nakao, Atsuto Inoue, Hiroaki Nomura, Tetsuya Kitamine, Manabu Fujita, Takeshi Nabe, Yoshiyuki Yamaura, Naoya Matsumura, Akira Imagawa, Yoshisuke Nakayama, Jun Takeuchi, Kazuyuki Ohmoto Discovery of Gemilukast (ONO-6950), a Dual CysLT1 and CysLT2 Antagonist As a Therapeutic Agent for Asthma J Med Chem. 2015 Aug 13;58(15):6093-113.
doi: 10.1021/acs.jmedchem.5b00741.
Epub 2015 Jul 22.
Cheryl de Vallière, Solange Vidal, Ieuan Clay, Giorgia Jurisic, Irina Tcymbarevich, Silvia Lang, Marie-Gabrielle Ludwig, Michal Okoniewski, Jyrki J. Eloranta, Gerd A. Kullak-Ublick, Carsten A. Wagner, Gerhard Rogler, Klaus Seuwen The pH-sensing receptor OGR1 improves barrier function of epithelial cells and inhibits migration in an acidic environment Am J Physiol Gastrointest Liver Physiol. 2015 Sep 15;309(6):G475-90.
doi: 10.1152/ajpgi.00408.2014.
Epub 2015 Jul 23.
Robert L. BertekapJr.; Neil T. Burford; Zhuyin Li; Andrew Alt High-Throughput Screening for Allosteric Modulators of GPCRs Methods Mol Biol. 2015;1335:223-40.
doi: 10.1007/978-1-4939-2914-6_15.
Emi Shoji, Hidetoshi Sakurai, Tokiko Nishino, Tatsutoshi Nakahata, Toshio Heike, Tomonari Awaya, Nobuharu Fujii, Yasuko Manabe, Masafumi Matsuo, Atsuko Sehara-Fujisawa Early pathogenesis of Duchenne muscular dystrophy modelled in patient-derived human induced pluripotent stem cells Sci Rep. 2015 Aug 20;5:12831.
doi: 10.1038/srep12831.
Yasuo Yonetomi, Tomohiko Sekioka, Michiaki Kadode, Tetsuya Kitamine, Akihiro Kamiya, Atsuto inoue, Takafumi Nakao, Hiroaki Nomura, Masayuki Murata, Shintaro Nakao, Fumio Nambu, Manabu Fujita, Shinji Nakade, Kazuhito Kawabata Effects of ONO-6950, a novel dual cysteinyl leukotriene 1 and 2 receptors antagonist, in a guinea pig model of asthma Eur J Pharmacol. 2015 Oct 15;765:242-8.
doi: 10.1016/j.ejphar.2015.08.041.
Epub 2015 Aug 28.
Atsushi Nakane, Yusuke Gotoh, Junji Ichihara, Hidetaka Nagata New screening strategy and analysis for identification of allosteric modulators for glucagon-like peptide-1 receptor using GLP-1 (9-36) amide Anal. Biochem. 2015 Dec 15;491:23-30.
doi: 10.1016/j.ab.2015.08.026.
Epub 2015 Sep 2.
Jae Wan Jang, Nam-Chul Cho, Sun-Joon Min, Yong Seo Cho, Ki Duk Park, Seon Hee Seo, Kyoung Tai No, Ae Nim Pae Novel Scaffold Identification of mGlu1 Receptor Negative Allosteric Modulators Using a Hierarchical Virtual Screening Approach Chem Biol Drug Des. 2016 Feb;87(2):239-56.
doi: 10.1111/cbdd.12654.
Epub 2015 Oct 9.
Yoshiharu Uruno, Yasuko Konishi, Atsushi Suwa, Kentaro Takai, Kengo Tojo, Tomokazu Nakako, Mutsuko Sakai, Takeshi Enomoto, Harumi Matsuda, Atsushi Kitamura, Takaaki Sumiyoshi Discovery of dihydroquinazolinone derivatives as potent, selective, and CNS-penetrant M1 and M4 muscarinic acetylcholine receptors agonists Bioorg Med Chem Lett. 2015 Nov 15;25(22):5357-61.
doi: 10.1016/j.bmcl.2015.09.032.
Epub 2015 Sep 12.
Tomohiko Sekioka, Michiaki Kadode, Masanori Fujii, Kazuhito Kawabata, Takashi Abe, Michiaki Horiba, Shigekatsu Kohno, Takeshi Nabe Expression of CysLT2 receptors in asthma lung, and their possible role in bronchoconstriction Allergol Int. 2015 Oct;64(4):351-8.
doi: 10.1016/j.alit.2015.04.008.
Epub 2015 Jun 3.
Brian Tomkowicz, Eileen Walsh, Adam Cotty, Raluca Verona, Nina Sabins, Fred Kaplan, Sandy Santulli-Marotto, Chen-Ni Chin, Jill Mooney, Russell B. Lingham, Michael Naso, Timothy McCabe TIM-3 Suppresses Anti-CD3/CD28-Induced TCR Activation and IL-2 Expression through the NFAT Signaling Pathway PLoS One. 2015 Oct 22;10(10):e0140694.
doi: 10.1371/journal.pone.0140694.
eCollection 2015.
Hilary Highfield Nickols, Joannes P. Yuh, Karen J. Gregory, Ryan D. Morrison, Brittney S. Bates, Shaun R. Stauffer, Kyle A. Emmitte, Michael Bubser, Weimin Peng, Michael T. Nedelcovych, Analisa Thompson, Xiaohui Lv, Zixiu Xiang, J. Scott Daniels, Colleen M. Niswender, Craig W. Lindsley, Carrie K. Jones,P. Jeffrey Conn VU0477573: Partial Negative Allosteric Modulator of the Subtype 5 Metabotropic Glutamate Receptor with In Vivo Efficacy J Pharmacol Exp Ther. 2016 Jan;356(1):123-36.
doi: 10.1124/jpet.115.226597.
Epub 2015 Oct 26.
Jesse A. May, Najam A. Sharif, Marsha A. McLaughlin, Hwang-Hsing Chen, Bryon S. Severns, Curtis R. Kelly, William F. Holt, Richard Young, Richard A. Glennon, Mark R. Hellberg, Thomas R. Dean Ocular Hypotensive Response in Nonhuman Primates of (8R)-1-[(2S)-2-Aminopropyl]-8,9-dihydro-7H-pyrano[2,3-g]indazol-8-ol a Selective 5-HT2Receptor Agonist J Med Chem. 2015 Nov 25;58(22):8818-33.
doi: 10.1021/acs.jmedchem.5b00857.
Epub 2015 Nov 9.
Hoang Nam Vu, Ji Young Kim, Ahmed H.E. Hassan, Kihang Choi Jong-Hyun Park, Ki Duk Park, Jae Kyun Lee, Ae Nim Pae, Hyunah Choo, Sun-Joon Min, Yong Seo Cho Synthesis and biological evaluation of picolinamides and thiazole-2-carboxamides as mGluR5 (metabotropic glutamate receptor 5) antagonists Bioorg Med Chem Lett. 2016 Jan 1;26(1):140-4.
doi: 10.1016/j.bmcl.2015.11.012.
Epub 2015 Nov 5.
Jennifer L. Herington, Daniel R. Swale, Naoko Brown, Elaine L. Shelton, Hyehun Choi, Charles H. Williams, Charles C. Hong, Bibhash C. Paria, Jerod S. Denton, Jeff Reese High-Throughput Screening of Myometrial Calcium-Mobilization to Identify Modulators of Uterine Contractility PLoS One. 2015 Nov 24;10(11):e0143243.
doi: 10.1371/journal.pone.0143243.
eCollection 2015.
Hai-bo Yu, Min Li, Wei-ping Wang, Xiao-liang Wang High throughput screening technologies for ion channels Acta Pharmacol Sin. 2016 Jan;37(1):34-43.
doi: 10.1038/aps.2015.108.
Epub 2015 Dec 14.
Abdallah Ahnaou, Hilde Lavreysen, Gary Tresadern, Jose M. Cid, Wilhelmus H. Drinkenburg mGlu2 Receptor Agonism, but Not Positive Allosteric Modulation, Elicits Rapid Tolerance towards Their Primary Efficacy on Sleep Measures in Rats PLoS One. 2015 Dec 11;10(12):e0144017.
doi: 10.1371/journal.pone.0144017.
eCollection 2015.
Hiroyuki Koyama, Hiroshi Iwakura, Katsuko Dote, Mika Bando, Hiroshi Hosoda, Hiroyuki Ariyasu, Toru Kusakabe, Choel Son, Kiminori Hosoda, Takashi Akamizu, Kenji Kangawa, Kazuwa Nakao Comprehensive Profiling of GPCR Expression in Ghrelin-producing Cells Endocrinology. 2016 Feb;157(2):692-704.
doi: 10.1210/en.2015-1784.
Epub 2015 Dec 15.
Sandra Santulli-Marotto, John Wheeler, Eilyn R. Lacy, Ken Boakye, Jennifer Luongo, Sheng-Jiun Wu, Mary Ryan CCL22-specific Antibodies Reveal That Engagement of Two Distinct Binding Domains on CCL22 Is Required for CCR4-mediated Function Monoclon Antib Immunodiagn Immunother. 2015 Dec;34(6):373-80.
doi: 10.1089/mab.2015.0039.
John Broad, Nobuyuki Takahashi, Masaomi Tajimi, Masaki Sudo, Adam Góralczyk, Umesh Parampalli, Kesava Mannur, Toshinori Yamamoto, Gareth J. Sanger RQ-00201894: A motilin receptor agonist causing long-lasting facilitation of human gastric cholinergically-mediated contractions J Pharmacol Sci. 2016 Feb;130(2):60-5.
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John Broad, Nobuyuki Takahashi, Masaomi Tajimi, Masaki Sudo, Adam Góralczyk, Umesh Parampalli, Kesava Mannur, Toshinori Yamamoto, Gareth J. Sanger RQ-00201894: A motilin receptor agonist causing long-lasting facilitation of human gastric cholinergically-mediated contractions J Pharmacol Sci. 2016 Feb;130(2):60-5.
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Haitao Ji, Jong-Ho Lee, Yugang Wang, Yilin Pang, Tao Zhang, Yan Xia, Lianjin Zhong, Jianxin Lyu, Zhimin Lu EGFR phosphorylates FAM129B to promote Ras activation Proc Natl Acad Sci U S A. 2016 Jan 19;113(3):644-9.
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2014
Authors Title Source
Anke Bill, Elizabeth M. Rosethorne, Toby C. Kent, Lindsay Fawcett, Lynn Burchell, Michiel T. van Diepen, Anthony Marelli, Sergey Batalov, Loren Miraglia, Anthony P. Orth, Nicole A. Renaud, Steven J. Charlton, Martin Gosling, L. Alex Gaither, Paul J. Groot-Kormelink High Throughput Mutagenesis for Identification of Residues Regulating Human Prostacyclin (hIP) Receptor Expression and Function PLoS One. 2014 Jun 2;9(6):e97973. doi: 10.1371/journal.pone.0097973. eCollection 2014.
Anke Bill, M. Oana Popa, Michiel T. van Diepen, Abraham Gutierrez, Sarah Lilley, Maria Velkova, Kathryn Acheson, Hedaythul Choudhury, Nicole A. Renaud, Douglas S. Auld, Martin Gosling, Paul J. Groot-Kormelink, L. Alex Gaither Variomics Screen Identifies the Re-entrant Loop of the Calcium-activated Chloride Channel ANO1 That Facilitates Channel Activation J Biol Chem. 2015 Jan 9;290(2):889-903. doi: 10.1074/jbc.M114.618140. Epub 2014 Nov 25.
Ann-Beth Nørholm, Pierre Francotte, Eric Goffin, Iuliana Botez, Laurence Danober, Pierre Lestage, Bernard Pirotte, Jette S. Kastrup, Lars Olsen, Chris Oostenbrink Thermodynamic Characterization of New Positive Allosteric Modulators Binding to the Glutamate Receptor A2 Ligand-Binding Domain: Combining Experimental and Computational Methods Unravels Differences in Driving Forces J Chem Inf Model. 2014 Dec 22;54(12):3404-16. doi: 10.1021/ci500559b. Epub 2014 Dec 9.
Anuradha Roy High Throughput Screening Operations at the University of Kansas Comb Chem High Throughput Screen. 2014 May;17(4):387-93.
Bin Cai, Xia Chen, Fang Liu, Jun Li, Lijuan Gu, Jason R. Liu, Jay Liu A Cell-Based Functional Assay Using a Green Fluorescent Protein-Based Calcium Indicator dCys-GCaMP Assay Drug Dev Technol. 2014 Aug;12(6):342-51. doi: 10.1089/adt.2014.584. Epub 2014 Aug 8.
Cheryse A. Furman, Rebecca A. Roof, Amy E. Moritz, Brittney N. Miller, Trevor B. Doyle, R. Benjamin Free, Ashwini K. Banala, Noel M. Paul, Vivek Kumar, Christopher D. Sibley, Amy Hauck Newman, David R. Sibley Investigation of the binding and functional properties of extended length D3 dopamine receptor-selective antagonists Eur Neuropsychopharmacol. 2014 Nov 29. pii: S0924-977X(14)00324-1. doi: 10.1016/j.euroneuro.2014.11.013. [Epub ahead of print]
Eunan Hendron, Xizhuo Wang, Yandong Zhou, Xiangyu Cai, Jun-Ichi Goto, Katsuhiko Mikoshiba, Yoshihiro Baba, Tomohiro Kurosaki, Youjun Wang, Donald L. Gill Potent functional uncoupling between STIM1 and Orai1 by dimeric 2-aminodiphenyl borinate analogs Cell Calcium. 2014 Oct 23;56(6):482-492. doi: 10.1016/j.ceca.2014.10.005. [Epub ahead of print]
Frederic Bassilana, Adam Carlson, Jennifer A DaSilva, Bianka Grosshans, Solange Vidal, Valerie Beck, Barbara Wilmeringwetter, Luis A Llamas, Todd B Showalter, Pascal Rigollier, Aaron Bourret, Arun Ramamurthy, Xu Wu, Fred Harbinski, Samantha Plonsky, Lac Lee, Heinz Ruffner, Paola Grandi, Markus Schirle, Jeremy Jenkins, Andreas W Sailer, Tewis Bouwmeester, Jeffrey A Porter, Vic Myer, Peter M Finan et al. Target identification for a Hedgehog pathway inhibitor reveals the receptor GPR39 Nat Chem Biol. 2014 May;10(5):343-9. doi: 10.1038/nchembio.1481. Epub 2014 Mar 16.
Hongkang Zhang, Beiyan Zou, Fang Du, Kaiping Xu, and Min Li Reporting Sodium Channel Activity Using Calcium Flux: Pharmacological Promiscuity of Cardiac Nav1.5 Mol Pharmacol. 2015 Feb;87(2):207-17. doi: 10.1124/mol.114.094789. Epub 2014 Nov 24.
Hyekyung P. Cho, Darren W. Engers, Daryl F. Venable, Colleen M. Niswender, Craig W. Lindsley, P. Jeffrey Conn, Kyle A. Emmitte, Alice L. Rodriguez A Novel Class of Succinimide-Derived Negative Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 1 Provides Insight into a Disconnect in Activity between the Rat and Human Receptors ACS Chem Neurosci. 2014 Jul 16;5(7):597-610. doi: 10.1021/cn5000343. Epub 2014 May 15.
Hyekyung P. Cho, Pedro M. Garcia-Barrantes, John T. Brogan, Corey R. Hopkins, Colleen M. Niswender, Alice L. Rodriguez, Daryl F. Venable, Ryan D. Morrison, Michael Bubser, J. Scott Daniels, Carrie K. Jones, P. Jeffrey Conn, Craig W. Lindsley Chemical Modulation of Mutant mGlu1 Receptors Derived from Deleterious GRM1 Mutations Found in Schizophrenics ACS Chem Biol. 2014 Oct 17;9(10):2334-46. doi: 10.1021/cb500560h. Epub 2014 Aug 28.
J. Kyle Bruner, Beiyan Zou, Hongkang Zhang, Yixin Zhang, Katharina Schmidt, Min Li Identification of novel small molecule modulators of K2P18.1 two-pore potassium channel Eur J Pharmacol. 2014 Oct 5;740:603-10. doi: 10.1016/j.ejphar.2014.06.021. Epub 2014 Jun 24.
Jesse E. Hanson, William J. Meilandt, Alvin Gogineni, Paul Reynen, James Herrington, Robby M. Weimer, Kimberly Scearce-Levie, Qiang Zhou Chronic GluN2B Antagonism Disrupts Behavior in Wild-Type Mice Without Protecting Against Synapse Loss or Memory Impairment in Alzheimer's Disease Mouse Models J Neurosci. 2014 Jun 11;34(24):8277-88. doi: 10.1523/JNEUROSCI.5106-13.2014.
John W. Kehoe, Brian Whitaker, Deidra Bethea, Eilyn R. Lacy, Ken Boakye, Sandra Santulli-Marotto, Mary H. Ryan, Yiqing Feng, John C. WheelerJohn W. Kehoe, Brian Whitaker, Deidra Bethea, Eilyn R. Lacy, Ken Boakye, Sandra Santulli-Marotto, Mary H. Ryan, Yiqing Feng, John C. Wheeler Isolation and optimization for affinity and biophysical characteristics of anti-CCL17 antibodies from the VH1-69 germline gene Protein Eng Des Sel. 2014 Jun;27(6):199-206. doi: 10.1093/protein/gzu012. Epub 2014 Apr 16.
Julie A. Meade, R. Benjamin Free, Nicole R. Miller, Lani S. Chun, Trevor B. Doyle, Amy E. Moritz, Jennie L. Conroy, Val J. Watts, David R. Sibley (-)-Stepholidine is a potent pan-dopamine receptor antagonist of both G protein- and β-arrestin-mediated signaling Psychopharmacology (Berl). 2014 Sep 18. [Epub ahead of print]
Junki Miyamoto, Taichi Mizukure, Si-Bum Park, Shigenobu Kishino, Ikuo Kimura, Kanako Hirano, Paolo Bergamo, Mauro Rossi, Takuya Suzuki, Makoto Arita, Jun Ogawa, Soichi Tanabe A gut microbial metabolite of linoleic acid, 10-hydroxy-cis-12-octadecenoic acid, ameliorates intestinal epithelial barrier impairment partially via GPR40/MEK-ERK pathway J Biol Chem. 2014 Dec 10. pii: jbc.M114.610733. [Epub ahead of print]
Kazuyuki Fukushima, Yoshikuni Tabata, Yoichi Imaizumi, Naohiro Kohmura, Michiko Sugawara, Kohei Sawada, Kazuto Yamazaki, Masashi Ito Characterization of Human Hippocampal Neural Stem/Progenitor Cells and Their Application to Physiologically Relevant Assays for Multiple Ionotropic Glutamate Receptors J Biomol Screen. 2014 Jun 30;19(8):1174-1184. [Epub ahead of print]
Laykea Tafesse, Toshiyuki Kanemasa, Noriyuki Kurose, Jianming Yu, Toshiyuki Asaki, Gang Wu, Yuka Iwamoto, Yoshitaka Yamaguchi, Chiyou Ni, John Engel, Naoki Tsuno, Aniket Patel, Xiaoming Zhou, Takuya Shintani, Kevin Brown, Tsuyoshi Hasegawa, Manjunath Shet, Yasuyoshi Iso, Akira Kato, Donald J. Kyle Structure–Activity Relationship Studies and Discovery of a Potent Transient Receptor Potential Vanilloid (TRPV1) Antagonist 4-[3-Chloro-5-[(1S)-1,2-dihydroxyethyl]-2-pyridyl]-N-[5-(trifluoromethyl)-2-pyridyl]-3,6-dihydro-2H-pyridine-1-carboxamide (V116517) as a Clinical Candidate for Pain Management J Med Chem. 2014 Aug 14;57(15):6781-94. doi: 10.1021/jm500818a. Epub 2014 Aug 1.
Lindsey C. Morris, Emily L. Days, Maxine Turney, Dehui Mi, Craig W. Lindsley, C. David Weaver, Kevin D. Niswender A Duplexed High-Throughput Screen to Identify Allosteric Modulators of the Glucagon-Like Peptide 1 and Glucagon Receptors J Biomol Screen. 2014 Feb 13;19(6):847-858. [Epub ahead of print]
Matthew F. Rouhier, Rene Raphemot, Jerod S. Denton, Peter M. Piermarini Pharmacological Validation of an Inward-Rectifier Potassium (Kir) Channel as an Insecticide Target in the Yellow Fever MosquitoAedes aegypti PLoS One. 2014 Jun 24;9(6):e100700. doi: 10.1371/journal.pone.0100700. eCollection 2014.
Michael P. Winters, Nalin Subasinghe, Mark Wall, Edward Beck, Michael R. Brandt, Michael F.A. Finley, Yi Liu, Mary Lou Lubin, Michael P. Neeper, Ning Qin, Christopher M. Flores, Zhihua Sui Discovery and SAR of novel tetrahydropyrrolo[3,4-c]pyrazoles as inhibitors of the N-type calcium channel Bioorg Med Chem Lett. 2014 May 1;24(9):2053-6. doi: 10.1016/j.bmcl.2014.03.062. Epub 2014 Mar 27.
Mikkel A. Rasmussen, Bjørn Holst, Zeynep Tümer, Mads G. Johnsen, Shuling Zhou, Tina C. Stummann, Poul Hyttel, Christian Clausen Transient p53 Suppression Increases Reprogramming of Human Fibroblasts without Affecting Apoptosis and DNA Damage Stem Cell Reports. 2014 Sep 9;3(3):404-13. doi: 10.1016/j.stemcr.2014.07.006. Epub 2014 Aug 21.
Mingfei Ji, Xubo Su, Xiaohong Su, Yingyi Chen, Wenkang Huang, Jian Zhang, Zhaobin Gao, Chuangang Li, Xuefeng Lu Identification of Novel Compounds for Human Bitter Taste Receptors Chem Biol Drug Des. 2014 Jul;84(1):63-74. doi: 10.1111/cbdd.12293. Epub 2014 Feb 28.
Nidhi Jalan-Sakrikar, Julie R. Field, Rebecca Klar, Margrith E. Mattmann, Karen J. Gregory, Rocio Zamorano, Darren W. Engers, Sean R. Bollinger, C. David Weaver, Emily L. Days, L. Michelle Lewis, Thomas J. Utley, Miguel Hurtado, Delphine Rigault, Francine Acher, Adam G. Walker, Bruce J. Melancon, Michael R. Wood, Craig W. Lindsley, P. Jeffrey Conn, Zixiu Xiang, Corey R. Hopkins, and Colleen M. Niswender Identification of Positive Allosteric Modulators VU0155094 (ML397) and VU0422288 (ML396) Reveals New Insights into the Biology of Metabotropic Glutamate Receptor 7 ACS Chem Neurosci. 2014 Dec 17;5(12):1221-37. doi: 10.1021/cn500153z. Epub 2014 Oct 9.
R. Benjamin Free, Lani S. Chun, Amy E. Moritz, Brittney N. Miller, Trevor B. Doyle, Jennie L. Conroy, Adrian Padron, Julie A. Meade, Jingbo Xiao, Xin Hu, Andrés E. Dulcey, Yang Han, Lihua Duan, Steve Titus, Melanie Bryant-Genevier, Elena Barnaeva, Marc Ferrer, Jonathan A. Javitch, Thijs Beuming, Lei Shi, Noel T. Southall, Juan J. Marugan, David R. Sibley Discovery and Characterization of a G Protein–Biased Agonist That Inhibits β-Arrestin Recruitment to the D2 Dopamine Receptor Mol Pharmacol. 2014 Jul;86(1):96-105. doi: 10.1124/mol.113.090563. Epub 2014 Apr 22.
Rene Raphemot, Matthew F. Rouhier, Daniel R. Swale, Emily Days, C. David Weaver, Kimberly M. Lovell, Leah C. Konkel, Darren W. Engers, Sean F. Bollinger, Corey Hopkins, Peter M. Piermarini , Jerod S. Denton Discovery and Characterization of a Potent and Selective Inhibitor of Aedes aegypti Inward Rectifier Potassium Channels PLoS One. 2014 Nov 6;9(11):e110772. doi: 10.1371/journal.pone.0110772. eCollection 2014.
Wendy J. Winchester, Katrina Gore, Sophie Glatt, Wendy Petit, Jennifer C. Gardiner, Kelly Conlon, Michael Postlethwaite, Pierre-Philippe Saintot, Sonia Roberts, James R. Gosset, Tomomi Matsuura, Mark D. Andrews, Paul A. Glossop, Michael J. Palmer, Nicola Clear, Susie Collins, Kevin Beaumont, David S. Reynolds Inhibition of TRPM8 Channels Reduces Pain in the Cold Pressor Test in Humans J Pharmacol Exp Ther. 2014 Nov;351(2):259-69. doi: 10.1124/jpet.114.216010. Epub 2014 Aug 14.
Zhiqiang Wang, Shimeng Liu, Miyo Kakizaki, Yuuki Hirose, Yukiko Ishikawa, Hiromasa Funato, Masashi Yanagisawa, Yonghao Yu, Qinghua Liu Orexin/Hypocretin Activates mTOR Complex 1 (mTORC1) via an Erk/Akt-independent and Calcium-stimulated Lysosome v-ATPase Pathway J Biol Chem. 2014 Nov 14;289(46):31950-9. doi: 10.1074/jbc.M114.600015. Epub 2014 Oct 2.
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2013
Authors Title Source
Andrew J. Storaska, Jian P. Mei, Meng Wu, Min Li, Susan M. Wade, Levi L. Blazer, Benita Sjögren, Corey R. Hopkins, Craig W. Lindsley, Zhihong Lin, Joseph J. Babcock, Owen McManus, Richard R. Neubig Reversible inhibitors of regulators of G-protein signaling identified in a high-throughput cell-based calcium signaling assay Cell Signal. 2013 Dec;25(12):2848-55. doi: 10.1016/j.cellsig.2013.09.007. Epub 2013 Sep 14.
C Brenneis, K Kistner, M Puopolo, S Jo, DP Roberson, M Sisignano, D Segal, E J Cobos, B J Wainger, S Labocha, N Ferreirós, C von Hehn, J Tran, G Geisslinger, P W Reeh, B P Bean, C J Woolf Bupivacaine-induced cellular entry of QX-314 and its contribution to differential nerve block Br J Pharmacol. 2014 Jan;171(2):438-51. doi: 10.1111/bph.12466.
Erica VanderPorten, Lauren Frick, Rebecca Turincio, Peter Thana, William LaMarr, Yichin Liu Label-free high-throughput assays to screen and characterize novel lactate dehydrogenase inhibitors Anal Biochem. 2013 Oct 15;441(2):115-22. doi: 10.1016/j.ab.2013.07.003. Epub 2013 Jul 16.
Florian P. M. Kohn High Throughput Fluorescent Screening of Membrane Potential and Intracellular Calcium Concentration Under Variable Gravity Conditions Microgravity Sci. Technol. 2013 April, Volume 25, Issue 2, pp 113-120. doi: 10.1007/s12217-012-9331-8
Hilde Lavreysen, Xavier Langlois, Abdel Ahnaou, Wilhelmus Drinkenburg, Paula te Riele, Ilse Biesmans, Ilse Van der Linden, Luc Peeters, Anton Megens, Cindy Wintmolders, Jose Maria Cid, Andrés A. Trabanco, Jose Ignacio Andrés, Frank M. Dautzenberg, Robert Lütjens, Gregor Macdonald, John R. Atack Pharmacological Characterization of JNJ-40068782, a New Potent, Selective, and Systemically Active Positive Allosteric Modulator of the mGlu2 Receptor and Its Radioligand [3H]JNJ-40068782 J Pharmacol Exp Ther. 2013 Sep;346(3):514-27. doi: 10.1124/jpet.113.204990. Epub 2013 Jun 13.
Jason T. Manka, Alice L. Rodriguez, Ryan D. Morrison, Daryl F. Venable, Hyekyung P. Cho, Anna L. Blobaum, J. Scott Daniels, Colleen M. Niswender, P. Jeffrey Conn, Craig W. Lindsley, Kyle A. Emmitte Octahydropyrrolo[3,4-c]pyrrole negative allosteric modulators of mGlu1 Bioorg Med Chem Lett. 2013 Sep 15;23(18):5091-6. doi: 10.1016/j.bmcl.2013.07.029. Epub 2013 Jul 23.
Kentaro Ozawa, Akira T. Komatsubara, Yuhei Nishimura, Tomoyo Sawada, Hiroto Kawafune, Hiroki Tsumoto, Yuichi Tsuji, Jing Zhao, Yoji Kyotani, Toshio Tanaka, Ryosuke Takahashi, Masanori Yoshizumi S-nitrosylation regulates mitochondrial quality control via activation of parkin Sci Rep. 2013;3:2202. doi: 10.1038/srep02202.
Kentaro Takai, Yasunao Inoue, Yasuko Konishi, Atsushi Suwa, Yoshiharu Uruno, Harumi Matsuda, Tomokazu Nakako, Mutsuko Sakai, Hiroyuki Nishikawa, Gakuji Hashimoto, Takeshi Enomoto, Atsushi Kitamura, Yasuaki Uematsu, Akihiko Kiyoshi, Takaaki Sumiyoshi Identification of N-substituted 8-azatetrahydroquinolone derivatives as selective and orally active M1 and M4 muscarinic acetylcholine receptors agonists Bioorg Med Chem Lett. 2013 Aug 15;23(16):4644-7. doi: 10.1016/j.bmcl.2013.06.013. Epub 2013 Jun 13.
Kimberly M. Lovell, Andrew S. Felts, Alice L. Rodriguez, Daryl F. Venable, Hyekyung P. Cho, Ryan D. Morrison, Frank W. Byers, J. Scott Daniels, Colleen M. Niswender, P. Jeffrey Conn, Craig W. Lindsley, Kyle A. Emmitte N-Acyl-N′-arylpiperazines as negative allosteric modulators of mGlu1: Identification of VU0469650, a potent and selective tool compound with CNS exposure in rats Bioorg Med Chem Lett. 2013 Jul 1;23(13):3713-8. doi: 10.1016/j.bmcl.2013.05.020. Epub 2013 May 17.
Lani S. Chun, R. Benjamin Free, Trevor B. Doyle, Xi-Ping Huang, Michele L. Rankin, David R. Sibley D1-D2 Dopamine Receptor Synergy Promotes Calcium Signaling via Multiple Mechanisms Mol Pharmacol. 2013 Aug;84(2):190-200. doi: 10.1124/mol.113.085175. Epub 2013 May 16.
Mamoru Tasakia, Miki Kobayashi, Yoshiyuki Tenda, Susumu Tsujimoto, Shoko Nakazato, Mako Numazaki, Yasuno Hirano, Hiroshi Matsuda, Tadashi Terasaka, Yasuhiro Miyao, Yasuaki Shimizu, Yoshitaka Hirayama Inhibition of antigen-induced airway inflammation and hyperresponsiveness in guinea pigs by a selective antagonist of “chemoattractant receptor homologous molecule expressed on Th2 cells” (CRTH2) Eur J Pharm Sci. 2013 Jun 14;49(3):434-40. doi: 10.1016/j.ejps.2013.04.017. Epub 2013 Apr 24.
Paul H. Tewson, Anne Marie Quinn, Thomas E. Hughes A Multiplexed Fluorescent Assay for Independent Second-Messenger Systems
Decoding GPCR Activation in Living Cells
J Biomol Screen. 2013 Aug;18(7):797-806. doi: 10.1177/1087057113485427. Epub 2013 Apr 11.
Rene Raphemot, C. David Weaver, Jerod S. Denton High-throughput Screening for Small-molecule Modulators of Inward Rectifier Potassium Channels J Vis Exp. 2013 Jan 27;(71). pii: 4209. doi: 10.3791/4209.
Rene Raphemot, Matthew F. Rouhier, Rocco D. Gogliotti, Kimberly M. Lovell, Rebecca M. Hine, Dhairyasheel Ghosalkar, Anthony Longo, Klaus W. Beyenbach, Jerod S. Denton, Peter M. Piermarini Eliciting Renal Failure in Mosquitoes with a Small-Molecule Inhibitor of Inward-Rectifying Potassium Channels PLoS One. 2013 May 29;8(5):e64905. doi: 10.1371/journal.pone.0064905. Print 2013.
Samarjit Patnaik, Juan J. Marugan, Ke Liu, Wei Zheng, Noel Southall, Seameen J. Dehdashti, Annika Thorsell, Markus Heilig, Lauren Bell, Michelle Zook, Bob Eskay, Kyle R. Brimacombe, Christopher P. Austin Structure–Activity Relationship of Imidazopyridinium Analogues as Antagonists of Neuropeptide S Receptor J Med Chem. 2013 Nov 27;56(22):9045-56. doi: 10.1021/jm400904m. Epub 2013 Nov 11.
Sandra Santulli-Marotto, Jamie Fisher, Theodore Petley, Ken Boakye, Tadas Panavas, Jennifer Luongo, Karl Kavalkovich, Michael Rycyzyn, Bingyuan Wu, Lester Gutshall, Ana Coelho, Cory M. Hogaboam, Mary Ryan Surrogate Antibodies That Specifically Bind and Neutralize CCL17 But Not CCL22 Monoclon Antib Immunodiagn Immunother. 2013 Jun;32(3):162-71. doi: 10.1089/mab.2012.0112.
Sandra Santulli-Marotto, Ken Boakye, Eilyn Lacy, Sheng-Jiun Wu, Jennifer Luongo, Karl Kavalkovich, Ana Coelho, Cory M. Hogaboam, Mary Ryan Engagement of Two Distinct Binding Domains on CCL17 Is Required for Signaling through CCR4 and Establishment of Localized Inflammatory Conditions in the Lung PLoS One. 2013 Dec 5;8(12):e81465. doi: 10.1371/journal.pone.0081465. eCollection 2013.
Sebastien Hannedouche, Valerie Beck, Juliet Leighton-Davies, Martin Beibel, Guglielmo Roma, Edward J. Oakeley, Vincent Lannoy, Jerome Bernard, Jacques Hamon, Samuel Barbieri, Inga Preuss, Marie-Christine Lasbennes, Andreas W. Sailer, Thomas Suply, Klaus Seuwen, Christian N. Parker, Frederic Bassilana Identification of the C3a Receptor (C3AR1) as the Target of the VGF-derived Peptide TLQP-21 in Rodent Cells J Biol Chem. 2013 Sep 20;288(38):27434-43. doi: 10.1074/jbc.M113.497214. Epub 2013 Aug 12.
Shoichiro Ozaki, Akinobu Z. Suzuki, Peter O. Bauer, Etsuko Ebisui, Katsuhiko Mikoshiba 2-Aminoethyl diphenylborinate (2-APB) analogues: Regulation of Ca2+ signaling Biochem Biophys Res Commun. 2013 Nov 15;441(2):286-90. doi: 10.1016/j.bbrc.2013.08.102. Epub 2013 Sep 11.
Summer E. Young, Matthew T. Duvernay, Michael L. Schulte, Craig W. Lindsley, Heidi E. Hamm Synthesis of Indole Derived Protease-Activated Receptor 4 Antagonists and Characterization in Human Platelets PLoS One. 2013 Jun 11;8(6):e65528. doi: 10.1371/journal.pone.0065528. Print 2013.
Susan J. Ramos-Hunter, Darren W. Engers, Kristian Kaufmann, Yu Du, Craig W. Lindsley, C. David Weaver, Gary A. Sulikowski Discovery and SAR of a novel series of GIRK1/2 and GIRK1/4 activators Bioorg Med Chem Lett. 2013 Sep 15;23(18):5195-8. doi: 10.1016/j.bmcl.2013.07.002. Epub 2013 Jul 18.
Thomas M. Bridges, Jerri M. Rook, Meredith J. Noetzel, Ryan D. Morrison, Ya Zhou, Rocco D. Gogliotti, Paige N. Vinson, Zixiu Xiang, Carrie K. Jones, Colleen M. Niswender, Craig W. Lindsley, Shaun R. Stauffer, P. Jeffrey Conn, J. Scott Daniels Biotransformation of a Novel Positive Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 5 Contributes to Seizure-Like Adverse Events in Rats Involving a Receptor Agonism-Dependent Mechanism Drug Metab Dispos. 2013 Sep;41(9):1703-14. doi: 10.1124/dmd.113.052084. Epub 2013 Jul 2.
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2012
Authors Title Source
Bo-Hye Im, Hyewhon Rhim GABAB receptor-mediated ERK1/2 phosphorylation via a direct interaction with CaV1.3 channels Neurosci Lett. 2012 Mar 28;513(1):89-94. doi: 10.1016/j.neulet.2012.02.014. Epub 2012 Feb 14.
Caroline Chambon, Claudia Jatzke, Nico Wegener, Andreas Gravius, Wojciech Danysz Using cholinergic M1 receptor positive allosteric modulators to improve memory via enhancement of brain cholinergic communication Eur J Pharmacol. 2012 Dec 15;697(1-3):73-80. doi: 10.1016/j.ejphar.2012.10.011. Epub 2012 Oct 17.
Christina Mølck, Kasper Harpsøe, David E. Gloriam, Rasmus P. Clausen, Ulf Madsen, Lars Ø. Pedersen, Hermogenes N. Jimenez, Søren M. Nielsen, Jesper M. Mathiesen, Hans Bräuner-Osborne Pharmacological Characterization and Modeling of the Binding Sites of Novel 1,3-Bis(pyridinylethynyl)benzenes as Metabotropic Glutamate Receptor 5-Selective Negative Allosteric Modulators Mol Pharmacol. 2012 Nov;82(5):929-37. doi: 10.1124/mol.112.078808. Epub 2012 Aug 16.
DAVID C. RINKER, PATRICK L. JONES, R. JASON PITTS, MICHAEL RUTZLER, GRAY CAMP, LUJUAN SUN, PINGXI XU, DANIEL C. DORSET, DAVID WEAVER, LAURENCE J. ZWIEBEL Novel high-throughput screens of Anopheles gambiae odorant receptors reveal candidate behaviour-modifying chemicals for mosquitoes Physiol Entomol. 2012;37:33–41 doi: 10.1111/j.1365-3032.2011.00821.x
Dinesh Puppala, Leon P. Collis, Sunny Z. Sun, Vinicius Bonato, Xian Chen, Blake Anson, Mathew Pletcher, Bernard Fermini, Sandra J. Engle Comparative Gene Expression Profiling in Human-Induced Pluripotent Stem Cell—Derived Cardiocytes and Human and Cynomolgus Heart Tissue Toxicol Sci. 2013 Jan;131(1):292-301. doi: 10.1093/toxsci/kfs282. Epub 2012 Sep 14.
Franck Potet, Amanda N. Lorinc, Sebastien Chaigne, Corey R. Hopkins, Raghav Venkataraman, Svetlana Z. Stepanovic, L. Michelle Lewis, Emily Days, Veniamin Y. Sidorov, Darren W. Engers, Beiyan Zou, David Afshartous, Alfred L. George Jr., Courtney M. Campbell, Jeffrey R. Balser, Min Li, Franz J. Baudenbacher, Craig W. Lindsley, C. David Weaver, Sabina Kupershmidt Identification and Characterization of a Compound That Protects Cardiac Tissue from Human Ether-à-go-go-related Gene (hERG)-related Drug-induced Arrhythmias J Biol Chem. 2012 Nov 16;287(47):39613-25. doi: 10.1074/jbc.M112.380162. Epub 2012 Oct 2.
Heinz Ruffner, Joëlle Sprunger, Olga Charlat, Juliet Leighton-Davies, Bianka Grosshans, Adrian Salathe, Svenja Zietzling, Valérie Beck, Maxime Therier, Andrea Isken, Yang Xie, Yue Zhang, Huaixiang Hao, Xiaoying Shi, Dong Liu, Qinhui Song, Ieuan Clay, Gabriele Hintzen, Jan Tchorz, Laure C. Bouchez, Gregory Michaud, Peter Finan, Vic E. Myer, Tewis Bouwmeester, Jeff Porter, Marc Hild, Fred Bassilana, Christian N. Parker, Feng Cong R-Spondin Potentiates Wnt/β-Catenin Signaling through Orphan Receptors LGR4 and LGR5 PLoS One. 2012;7(7):e40976. doi: 10.1371/journal.pone.0040976. Epub 2012 Jul 16.
India C. Severin, Adriano L.S. Souza, Jonathan H. Davis, Najia Musolino, Matthias Mack, Christine A. Power, Amanda E.I. Proudfoot Properties of 7ND–CCL2 are modulated upon fusion to Fc Protein Eng Des Sel. 2012 May;25(5):213-22. doi: 10.1093/protein/gzs008. Epub 2012 Mar 2.
Jack Bergman, Rebecca A. Roof, Cheryse A. Furman, Jennie L. Conroy, Nancy K. Mello, David R. Sibley, Phil Skolnick Modification of cocaine self-administration by buspirone (buspar®): potential involvement of D3 and D4 dopamine receptors Int J Neuropsychopharmacol. 2013 Mar;16(2):445-58. doi: 10.1017/S1461145712000661. Epub 2012 Jul 25.
James M. Salovich, Paige N. Vinson, Douglas J. Sheffler, Atin Lamsal, Thomas J. Utley, Anna L. Blobaum, Thomas M. Bridges, Uyen Le, Carrie K. Jones, Michael R. Wood, J. Scott Daniels, P. Jeffrey Conn, Colleen M. Niswender, Craig W. Lindsley, Corey R. Hopkins Discovery of N-(4-methoxy-7-methylbenzo[d]thiazol-2-yl)isonicatinamide, ML293, as a novel, selective and brain penetrant positive allosteric modulator of the muscarinic 4 (M4) receptor Bioorg Med Chem Lett. 2012 Aug 1;22(15):5084-8. doi: 10.1016/j.bmcl.2012.05.109. Epub 2012 Jun 6.
Jingbo Xiao, R. Benjamin Free, Elena Barnaeva, Jennie Conroy, Trevor Doyle, Marthe Bryant-Genevier, Mercedes K. Taylor, Noel Southall, Xin Hu, Marc Ferrer, Steve Titus, Wei Zheng, David R. Sibley, Juan J. Marugan. Discovery, optimization, and characterization of a novel series of dopamine D2 versus D3 receptor selective antagonists Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-. 2012 Dec 25 [updated 2013 Sep 03].
Jung-eun Park, Wan Keun Ji, Jae Wan Jang, Ae Nim Pae, Keehyun Choi, Ki Hang Choi, Jahyo Kang, Eun Joo Roh Synthesis and biological evaluation of 1-(2-hydroxy-3-phenyloxypropyl)piperazine derivatives as T-type calcium channel blockers Bioorg Med Chem Lett. 2013 Mar 15;23(6):1887-90. doi: 10.1016/j.bmcl.2012.12.072. Epub 2013 Jan 12.
Jutty Rajan Prashanth, Richard J. Lewis, Sébastien Dutertre Towards an integrated venomics approach for accelerated conopeptide discovery Toxicon. 2012 Sep 15;60(4):470-7. doi: 10.1016/j.toxicon.2012.04.340. Epub 2012 Apr 28.
Linjie Chen, Lili Jin, Naiming Zhou An update of novel screening methods for GPCR in drug discovery Expert Opin Drug Discov. 2012 Sep;7(9):791-806. doi: 10.1517/17460441.2012.699036. Epub 2012 Jun 21.
Mohammed Akhlaq; Elizabeth M. Rosethorne; Afrah Sattikar; Toby C. Kent The Use of Cold Plasma Technology to Reduce Carryover in Screening Assays J Lab Autom. 2013 Aug;18(4):269-75. doi: 10.1177/2211068212457780. Epub 2012 Sep 14.
Nalin L. Subasinghe, Mark J. Wall, Michael P. Winters, Ning Qin, Mary Lou Lubin, Michael F.A. Finley, Michael R. Brandt, Michael P. Neeper, Craig R. Schneider, Raymond W. Colburn, Christopher M. Flores, Zhihua Sui A novel series of pyrazolylpiperidine N-type calcium channel blockers Bioorg Med Chem Lett. 2012 Jun 15;22(12):4080-3. doi: 10.1016/j.bmcl.2012.04.075. Epub 2012 May 2.
Roman Hudec, Kozo Hamada, Katsuhiko Mikoshiba A fluorescence-based assay for the measurement of S-adenosylhomocysteine hydrolase activity in biological samples Anal Biochem. 2013 Feb 15;433(2):95-101. doi: 10.1016/j.ab.2012.10.014. Epub 2012 Oct 15.
Shen Yin, Rocio Zamorano, P. Jeffrey Conn, Colleen M. Niswender Functional selectivity induced by mGlu4 receptor positive allosteric modulation and concomitant activation of Gq coupled receptors Neuropharmacology. 2013 Mar;66:122-32. doi: 10.1016/j.neuropharm.2012.03.003. Epub 2012 Mar 9.
Shuzo Watanabe Discovery of voltage-gated sodium-channel blockers for the treatment of neuropathic pain Nihon Yakurigaku Zasshi. 2012 Nov;140(5):201-5. doi: 10.1254/fpj.140.201
Wenthur C, Daniels JS, Morrison R, Engers JL, Niswender CM, Conn PJ, Lindsley CW. Development of a Second Generation mGlu3 NAM Probe Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-. 2012 Dec 10 [updated 2013 Mar 22].
Yueming Zheng, Xuejing Zhu, Pingzheng Zhou, Xi Lan, Haiyan Xu, Min Li, Zhaobing Gao Hexachlorophene Is a Potent KCNQ1/KCNE1 Potassium Channel Activator Which Rescues LQTs Mutants PLoS One. 2012;7(12):e51820. doi: 10.1371/journal.pone.0051820. Epub 2012 Dec 12.
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2011
Authors Title Source
Atsushi Inayoshi, Yoshiyuki Sugimoto, Jun Funahashi, Saori Takahashi, Masahiro Matsubara, Hideaki Kusaka Mechanism underlying the block of human Cav3.2 T-type Ca2+ channels by benidipine, a dihydropyridine Ca2+ channel blocker Life Sci. 2011 May 9;88(19-20):898-907. doi: 10.1016/j.lfs.2011.03.019. Epub 2011 Apr 3.
C. David Weaver Triple-Addition Assay Protocols for Detecting and Characterizing Modulators of Seven-Transmembrane Receptors Curr Protoc Chem Biol. 2011 Sep 1;3(3):119-40. doi: 10.1002/9780470559277.ch110060.
Carrie K. Jones, Michael Bubser, Analisa D. Thompson, Jonathan W. Dickerson, Nathalie Turle-Lorenzo, Marianne Amalric, Anna L. Blobaum, Thomas M. Bridges, Ryan D. Morrison, Satyawan Jadhav, Darren W. Engers, Kimberly Italiano, Jacob Bode, J. Scott Daniels, Craig W. Lindsley, Corey R. Hopkins, P. Jeffrey Conn, Colleen M. Niswender The Metabotropic Glutamate Receptor 4-Positive Allosteric Modulator VU0364770 Produces Efficacy Alone and in Combination with L-DOPA or an Adenosine 2A Antagonist in Preclinical Rodent Models of Parkinson's Disease J Pharmacol Exp Ther. 2012 Feb;340(2):404-21. doi: 10.1124/jpet.111.187443. Epub 2011 Nov 16.
Curtis A. Thorne, Bonnie Lafleur, Michelle Lewis, Alison J. Hanson, Kristin K. Jernigan, David C. Weaver, Kari A. Huppert, Tony W. Chen, Chonlarat Wichadiit, Christopher S. Cselenyi, Emilios Tahinci, Kelly C. Meyers, Emily Waskow, Darren Orton, Adrian Salic, Laura A. Lee, David J. Robbins, Stacey S. Huppert, Ethan Lee A Biochemical Screen for Identification of Small-Molecule Regulators of the Wnt Pathway Using Xenopus Egg Extracts J Biomol Screen. 2011 Oct;16(9):995-1006. doi: 10.1177/1087057111416657. Epub 2011 Aug 21.
Gaëlle Dintilhac, Deniz Arslan, Sébastien Dilly, Laurence Danober, Iuliana Botez, Pierre Lestage, Bernard Pirotte, Pascal de Tullio New substituted aryl esters and aryl amides of 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxides as positive allosteric modulators of AMPA receptors Med. Chem. Commun., 2011,2, 509-523 doi: 10.1039/C1MD00069A
Haibo Yu, Meng Wu, Corey Hopkins, Julie Engers, Steve Townsend, Craig Lindsley, Owen B McManus, Min Li. A small molecule activator of KCNQ2 and KCNQ4 channels. Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-. 2011 Mar 29 [updated 2013 Feb 28].
Haibo Yu, Kaiping Xu, Beiyan Zou, Meng Wu, Owen B. McManus, Julie Le Engers, Yiu-Yin Cheung, James M. Salovich, Corey R. Hopkins, Craig W. Lindsley, and Min Li. Identification of a novel, small molecule inhibitor of KCNQ2 channels Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-. 2011 Oct 28 [updated 2013 Feb 25].
Haibo Yu, Zhihong Lin, Kaiping Xu, Xiaofang Huang, Shunyou Long, Meng Wu, Owen B. McManus, Julie Le Engers, Margrith E. Mattmann, Darren W. Engers, Uyen M. Le, Craig W. Lindsley, Corey R. Hopkins,  Min Li. Identification of a novel, small molecule activator of KCNQ1 channels Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-. 2011 Dec 16 [updated 2013 Mar 7].
Jacques Pantela, Savannah Y. Williams, Dehui Mi, Julien Sebag, Jackie D. Corbin, C. David Weaver, Roger D. Cone Development of a high throughput screen for allosteric modulators of melanocortin-4 receptor signaling using a real time cAMP assay Eur J Pharmacol. 2011 Jun 11;660(1):139-47. doi: 10.1016/j.ejphar.2011.01.031. Epub 2011 Feb 4.
Jinghai Song, Hiroshi Hagiya, Haruto Kurata, Hirotaka Mizuno, Toshinori Ito Prevention of GVHD and graft rejection by a new S1P receptor agonist, W-061, in rat small bowel transplantation Transpl Immunol. 2012 Mar;26(2-3):163-70. doi: 10.1016/j.trim.2011.12.005. Epub 2011 Dec 14.
Jun Chen, Regina M. Reilly, Philip R. Kym, and Shailen Joshi. In Vitro and in Vivo Assays for the Discovery of Analgesic Drugs Targeting TRP Channels In: Zhu MX, editor. TRP Channels. Boca Raton (FL): CRC Press; 2011. Chapter 18.
Marianthi Papakosta, Carine Dalle, Alison Haythornthwaite, Lishuang Cao, Edward B. Stevens, Gillian Burgess, Rachel Russell, Peter J. Cox, Stephen C. Phillips, Christian Grimm The Chimeric Approach Reveals That Differences in the TRPV1 Pore Domain Determine Species-specific Sensitivity to Block of Heat Activation J Biol Chem. 2011 Nov 11;286(45):39663-72. doi: 10.1074/jbc.M111.273581. Epub 2011 Sep 12.
Menghang Xia, Sampada A. Shahane, Ruili Huang, Steven A. Titus, Enoch Shum, Yong Zhao, Noel Southall, Wei Zheng, Kristine L. Witt, Raymond R. Tice, Christopher P. Austin Identification of quaternary ammonium compounds as potent inhibitors of hERG potassium channels Toxicol Appl Pharmacol. 2011 May 1;252(3):250-8. doi: 10.1016/j.taap.2011.02.016. Epub 2011 Feb 26.
Meredith J Noetzel, Jerri M Rook, Paige N Vinson, Hyekyung Cho, Emily Days, Y Zhou, Alice L Rodriguez, Hilde Lavreysen, Shaun R Stauffer, Colleen M Niswender, Zixiu Xiang, J Scott Daniels, Crag W Lindsley, C David Weaver, P Jeffrey Conn Functional Impact of Allosteric Agonist Activity of Selective Positive Allosteric Modulators of mGlu5 in Regulating CNS Function Mol Pharmacol. 2012 Feb;81(2):120-33. doi: 10.1124/mol.111.075184. Epub 2011 Oct 21.
Peter R McDonald, Anuradha Roy, Rathnam Chaguturu The University of Kansas High-Throughput Screening Laboratory. Part II: enabling collaborative drug-discovery partnerships through cutting-edge screening technology Future Med Chem. 2011 Jul;3(9):1101-10. doi: 10.4155/fmc.11.84.
Rene Raphemot, Daniel F. Lonergan, Thuy T. Nguyen, Thomas Utley, L. Michelle Lewis, Rishin Kadakia, C. David Weaver, Rocco Gogliotti, Corey Hopkins, Craig W. Lindsley, Jerod S. Denton Discovery, characterization, and structure–activity relationships of an inhibitor of inward rectifier potassium (Kir) channels with preference for Kir2.3, Kir3.X, and Kir7.1 Front Pharmacol. 2011 Nov 30;2:75. doi: 10.3389/fphar.2011.00075. eCollection 2011.
Thierry Ferain, Hamid Hoveyda, Frédéric Ooms, Dominique Schols, Jérôme Bernard, Graeme Fraser Agonist-Induced Internalization of CC Chemokine Receptor 5 as a Mechanism to Inhibit HIV Replication J Pharmacol Exp Ther. 2011 Jun;337(3):655-62. doi: 10.1124/jpet.111.179622. Epub 2011 Mar 9.
Xinmin Xie, John T. Brogan, Michael L. Schulte, Debbie Mi, Haibo Yu, Eric S. Dawson, Min Li, Owen McManus, Julie Engers, L. Michelle Lewis, Analisa Thompson, Carrie K. Jones, C. David Weaver, Craig W. Lindsley. Scaffold Hopping Affords a Highly Selective in vitro and in vivo T-Type Calcium Inhibitor Probe Free From IP Issues Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-. 2011 Mar 31 [updated 2013 Mar 22].
Yasuaki Sanada, Tsunekazu Mizushima, Yasuyuki Kai, Junichi Nishimura, Hiroshi Hagiya, Haruto Kurata, Hirotaka Mizuno, Etsuko Uejima, Toshinori Ito Therapeutic Effects of Novel Sphingosine-1-Phosphate Receptor Agonist W-061 in Murine DSS Colitis PLoS One. 2011;6(9):e23933. doi: 10.1371/journal.pone.0023933. Epub 2011 Sep 8.
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2010
Authors Title Source
Ke Liu, Noel Southall, Steve A. Titus, James Inglese, Robert L. Eskay, Paul Shinn, Christopher P. Austin, Markus A. Heilig and Wei Zheng. A Multiplex Calcium Assay for Identification of GPCR Agonists and Antagonists Assay Drug Dev Technol. 2010 Jun;8(3):367-79.
Brad P. Barnett, Yousang Hwang, Martin S. Taylor, Henriette Kirchner, Paul T. Pfluger, Vincent Bernard, Yu-yi Lin, Erin M. Bowers, Chandrani Mukherjee, Woo-Jin Song, Patti A. Longo, Daniel J. Leahy, Mehboob A. Hussain, Matthias H. Tschöp, Jef D. Boeke and Philip A. Cole. Glucose and Weight Control in Mice with a Designed Ghrelin O-Acyltransferase Inhibitor Science 17 December 2010: Vol. 330 no. 6011 pp. 1689-1692.
Evan P Lebois, Thomas M Bridges, L. Michelle Lewis, Eric S Dawson, Alexander S. Kane, Zixiu Xiang, Satyawan B Jadhav, Huiyong Yin, J. Phillip Kennedy, Jens Meiler, Colleen M. Niswender, Carrie K Jones, P Jeffrey Conn, C David Weaver, and Craig W Lindsley. Discovery and characterization of novel subtype-selective allosteric agonists for the investigation of M1 receptor function in the central nervous system ACS Chem Neurosci. 2010; 1(2): 104-121.
Zhaobing Gao, Tangzhi Zhang, Meng Wu, Qiaojie Xiong, Haiyan Sun, Yinan Zhang, Liansuo Zu, Wei Wang and Min Li Isoform-specific Prolongation of Kv7 (KCNQ) Potassium Channel Opening Mediated by New Molecular Determinants for Drug-Channel Interactions September 3, 2010 The Journal of Biological Chemistry, 285, 28322-28332.
Jinliang Sui, Shakira Cotard, Jennifer Andersen, Ping Zhu, Jane Staunton, Margaret Lee, and Stephen Lin. Isoform-specific Prolongation of Kv7 (KCNQ) Potassium Channel Opening Mediated by New Molecular Determinants for Drug-Channel Interactions ASSAY and Drug Development Technologies. December 2010, 8(6): 656-668. doi:10.1089/adt.2010.0312.
Stephen Lin, Jinliang Sui, Shakira Cotard, Brenda Fung, Jennifer Andersen, Ping Zhu, Najib El Messadi, Joseph Lehar, Margaret Lee, and Jane Staunton. Identification of Synergistic Combinations of F508del Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Modulators ASSAY and Drug Development Technologies. December 2010, 8(6): 669-684. doi:10.1089/adt.2010.0313.
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2009
Authors Title Source
Delpire E, Days E, Lewis LM, Mi D, Kim K, Lindsley CW, Weaver CD. Small-molecule screen identifies inhibitors of the neuronal K-Cl cotransporter KCC2 Proc Natl Acad Sci U S A. 2009 Mar 31;106(13):5383-8. Epub 2009 Mar 11.
Irukayama-Tomobe Y, Tanaka H, Yokomizo T, Hashidate-Yoshida T, Yanagisawa M, Sakurai T. Aromatic D-amino acids act as chemoattractant factors for human leukocytes through a G protein-coupled receptor, GPR109B Proc Natl Acad Sci U S A. 2009 Mar 10;106(10):3930-4. Epub 2009 Feb 23.
Lewis LM, Bhave G, Chauder BA, Banerjee S, Lornsen KA, Redha R, Fallen K, Lindsley CW, Weaver CD, Denton JS. High-throughput screening reveals a small-molecule inhibitor of the renal outer medullary potassium channel and Kir7.1 Mol Pharmacol. 2009 Nov;76(5):1094-103. Epub 2009 Aug 25.
Marlo JE, Niswender CM, Days EL, Bridges TM, Xiang Y, Rodriguez AL, Shirey JK, Brady AE, Nalywajko T, Luo Q, Austin CA, Williams MB, Kim K, Williams R, Orton D, Brown HA, Lindsley CW, Weaver CD, Conn PJ. Discovery and characterization of novel allosteric potentiators of M1 muscarinic receptors reveals multiple modes of activity Mol Pharmacol. 2009 Mar;75(3):577-88. Epub 2008 Dec 1.
Sheffler DJ, Williams R, Bridges TM, Xiang Z, Kane AS, Byun NE, Jadhav S, Mock MM, Zheng F, Lewis LM, Jones CK, Niswender CM, Weaver CD, Lindsley CW, Conn PJ. A novel selective muscarinic acetylcholine receptor subtype 1 antagonist reduces seizures without impairing hippocampus-dependent learning Mol Pharmacol. 2009 Aug;76(2):356-68. Epub 2009 Apr 30.
Shirey JK, Brady AE, Jones PJ, Davis AA, Bridges TM, Kennedy JP, Jadhav SB, Menon UN, Xiang Z, Watson ML, Christian EP, Doherty JJ, Quirk MC, Snyder DH, Lah JJ, Levey AI, Nicolle MM, Lindsley CW, Conn PJ. A selective allosteric potentiator of the M1 muscarinic acetylcholine receptor increases activity of medial prefrontal cortical neurons and restores impairments in reversal learning J Neurosci. 2009 Nov 11;29(45):14271-86.
Bridges TM, Marlo JE, Niswender CM, Jones CK, Jadhav SB, Gentry PR, Plumley HC, Weaver CD, Conn PJ, Lindsley CW. Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins J Med Chem. 2009 Jun 11;52(11):3445-8.
Engers DW, Niswender CM, Weaver CD, Jadhav S, Menon UN, Zamorano R, Conn PJ, Lindsley CW, Hopkins CR. Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs) J Med Chem. 2009 Jul 23;52(14):4115-8.
Sharma S, Kedrowski J, Rook JM, Smith RL, Jones CK, Rodriguez AL, Conn PJ, Lindsley CW. Discovery of molecular switches that modulate modes of metabotropic glutamate receptor subtype 5 (mGlu5) pharmacology in vitro and in vivo within a series of functionalized, regioisomeric 2- and 5-(phenylethynyl)pyrimidines J Med Chem. 2009 Jul 23;52(14):4103-6.
Wise H, Abel PW, Cawkill D. Use of reduced temperature cell pausing to enhance flexibility of cell-based assays J Biomol Screen. 2009 Jul;14(6):716-22. Epub 2009 May 21.
Mori T, Itami S, Yanagi T, Tatara Y, Takamiya M, Uchida T. Use of a real-time fluorescence monitoring system for high-throughput screening for prolyl isomerase inhibitors J Biomol Screen. 2009 Apr;14(4):419-24.
Weaver CD, Sheffler DJ, Lewis LM, Bridges TM, Williams R, Nalywajko NT, Kennedy JP, Mulder MM, Jadhav S, Aldrich LA, Jones CK, Marlo JE, Niswender CM, Mock MM, Zheng F, Conn PJ, Lindsley CW. Discovery and development of a potent and highly selective small molecule muscarinic acetylcholine receptor subtype I (mAChR 1 or M1) antagonist in vitro and in vivo probe Curr Top Med Chem. 2009;9(13):1217-26.
Kim Y, Kang S, Lee JY, Rhim H. High throughput screening assay of alpha(1G) T-type Ca2+ channels and comparison with patch-clamp studies Comb Chem High Throughput Screen. 2009 Mar;12(3):296-302.
Williams R, Johnson KA, Gentry PR, Niswender CM, Weaver CD, Conn PJ, Lindsley CW, Hopkins CR. Synthesis and SAR of a novel positive allosteric modulator (PAM) of the metabotropic glutamate receptor 4 (mGluR4) Bioorg Med Chem Lett. 2009 Sep 1;19(17):4967-70. Epub 2009 Jul 18.
Rodriguez AL, Williams R, Zhou Y, Lindsley SR, Le U, Grier MD, Weaver CD, Conn PJ, Lindsley CW. Discovery and SAR of novel mGluR5 non-competitive antagonists not based on an MPEP chemotype Bioorg Med Chem Lett. 2009 Jun 15;19(12):3209-13. Epub 2009 May 3.
Williams R, Niswender CM, Luo Q, Le U, Conn PJ, Lindsley CW. Positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4). Part II: Challenges in hit-to-lead Bioorg Med Chem Lett. 2009 Feb 1;19(3):962-6. Epub 2008 Dec 25.
Felts AS, Saleh SA, Le U, Rodriguez AL, Weaver CD, Conn PJ, Lindsley CW, Emmitte KA. Discovery and SAR of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of mGlu5 Bioorg Med Chem Lett. 2009 Dec 1;19(23):6623-6. Epub 2009 Oct 9.
Zhou Y, Rodriguez AL, Williams R, Weaver CD, Conn PJ, Lindsley CW. Synthesis and SAR of novel, non-MPEP chemotype mGluR5 NAMs identified by functional HTS Bioorg Med Chem Lett. 2009 Dec 1;19(23):6502-6. Epub 2009 Oct 28.
Titus SA, Beacham D, Shahane SA, Southall N, Xia M, Huang R, Hooten E, Zhao Y, Shou L, Austin CP, Zheng W. A new homogeneous high-throughput screening assay for profiling compound activity on the human ether-a-go-go-related gene channel Anal Biochem. 2009 Nov 1;394(1):30-8. Epub 2009 Jul 5.
Lin Tian, S. Andrew Hires, Tianyi Mao, Daniel Huber, M. Eugenia Chiappe, Sreekanth H. Chalasani, Leopoldo Petreanu, Jasper Akerboom, Sean A. McKinney, Eric R. Schreiter, Cornelia I. Bargmann, Vivek Jayaraman, Karel Svoboda, and Loren L. Looger Imaging neural activity in worms, flies and mice with improved GCaMP calcium indicators "Nat Methods. 2009 December; 6(12): 875–881.Published online 2009 November 8. doi: 10.1038/nmeth.1398"
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2008
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Taniguchi Y, Tonai-Kachi H, Shinjo K. 5-Nitro-2-(3-phenylpropylamino)benzoic acid is a GPR35 agonist Pharmacology. 2008;82(4):245-9. Epub 2008 Sep 26.
Ayala JE, Niswender CM, Luo Q, Banko JL, Conn PJ. Group III mGluR regulation of synaptic transmission at the SC-CA1 synapse is developmentally regulated Neuropharmacology. 2008 Apr;54(5):804-14. Epub 2007 Dec 24.
Shirey JK, Xiang Z, Orton D, Brady AE, Johnson KA, Williams R, Ayala JE, Rodriguez AL, Wess J, Weaver D, Niswender CM, Conn PJ. An allosteric potentiator of M4 mAChR modulates hippocampal synaptic transmission Nat Chem Biol. 2008 Jan;4(1):42-50. Epub 2007 Dec 2.
Niswender CM, Johnson KA, Weaver CD, Jones CK, Xiang Z, Luo Q, Rodriguez AL, Marlo JE, de Paulis T, Thompson AD, Days EL, Nalywajko T, Austin CA, Williams MB, Ayala JE, Williams R, Lindsley CW, Conn PJ. Discovery, characterization, and antiparkinsonian effect of novel positive allosteric modulators of metabotropic glutamate receptor 4 Mol Pharmacol. 2009 Mar;75(3):577-88. Epub 2008 Dec 1.
Niswender CM, Johnson KA, Luo Q, Ayala JE, Kim C, Conn PJ, Weaver CD. A novel assay of Gi/o-linked G protein-coupled receptor coupling to potassium channels provides new insights into the pharmacology of the group III metabotropic glutamate receptors Mol Pharmacol. 2008 Apr;73(4):1213-24. Epub 2008 Jan 2.
Kobayashi K, Nishizawa Y, Sawada K, Ogura H, Miyabe M. K(+)-channel openers suppress epileptiform activities induced by 4-aminopyridine in cultured rat hippocampal neurons J Pharmacol Sci. 2008 Dec;108(4):517-28. Epub 2008 Dec 11.
Jones CK, Brady AE, Davis AA, Xiang Z, Bubser M, Tantawy MN, Kane AS, Bridges TM, Kennedy JP, Bradley SR, Peterson TE, Ansari MS, Baldwin RM, Kessler RM, Deutch AY, Lah JJ, Levey AI, Lindsley CW, Conn PJ. Novel selective allosteric activator of the M1 muscarinic acetylcholine receptor regulates amyloid processing and produces antipsychotic-like activity in rats J Neurosci. 2008 Oct 8;28(41):10422-33.
Akasofu S, Sawada K, Kosasa T, Hihara H, Ogura H, Akaike A. Donepezil attenuates excitotoxic damage induced by membrane depolarization of cortical neurons exposed to veratridine Eur J Pharmacol. 2008 Jul 7;588(2-3):189-97. Epub 2008 Apr 13.
Gunnet JW, Wines P, Xiang M, Rybczynski P, Andrade-Gordon P, de Garavilla L, Parry TJ, Cheung WM, Minor L, Demarest KT, Maryanoff BE, Damiano BP. Pharmacological characterization of RWJ-676070, a dual vasopressin V(1A)/V(2) receptor antagonis Eur J Pharmacol. 2008 Aug 20;590(1-3):333-42. Epub 2008 Jun 7.
Kim HJ, Yun HM, Kim T, Nam G, Roh EJ, Kostenis E, Choo HY, Pae AN, Rhim H. Functional human 5-HT6 receptor assay for high throughput screening of chemical ligands and binding proteins Comb Chem High Throughput Screen. 2008 May;11(4):316-24.
Niswender CM, Lebois EP, Luo Q, Kim K, Muchalski H, Yin H, Conn PJ, Lindsley CW. Positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4): Part I. Discovery of pyrazolo[3,4-d]pyrimidines as novel mGluR4 positive allosteric modulators Bioorg Med Chem Lett. 2008 Oct 15;18(20):5626-30. Epub 2008 Aug 29.
Lewis LM, Sheffler D, Williams R, Bridges TM, Kennedy JP, Brogan JT, Mulder MJ, Williams L, Nalywajko NT, Niswender CM, Weaver CD, Conn PJ, Lindsley CW. Synthesis and SAR of selective muscarinic acetylcholine receptor subtype 1 (M1 mAChR) antagonists Bioorg Med Chem Lett. 2008 Feb 1;18(3):885-90. Epub 2008 Jan 4.
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2007
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McNamara CR, Mandel-Brehm J, Bautista DM, Siemens J, Deranian KL, Zhao M, Hayward NJ, Chong JA, Julius D, Moran MM, Fanger CM. TRPA1 mediates formalin-induced pain Proc Natl Acad Sci U S A. 2007 Aug 14;104(33):13525-30. Epub 2007 Aug 8.
Hemstapat K, Da Costa H, Nong Y, Brady AE, Luo Q, Niswender CM, Tamagnan GD, Conn PJ. A novel family of potent negative allosteric modulators of group II metabotropic glutamate receptors J Pharmacol Exp Ther. 2007 Jul;322(1):254-64. Epub 2007 Apr 6.
Song F, Lu S, Gunnet J, Xu JZ, Wines P, Proost J, Liang Y, Baumann C, Lenhard J, Murray WV, Demarest KT, Kuo GH. Synthesis and biological evaluation of 3-aryl-3-(4-phenoxy)-propionic acid as a novel series of G protein-coupled receptor 40 agonists J Med Chem. 2007 Jun 14;50(12):2807-17. Epub 2007 May 15.
Cassutt KJ, Orsini MJ, Abousleiman M, Colone D, Tang W. Identifying nonselective hits from a homogeneous calcium assay screen J Biomol Screen. 2007 Mar;12(2):285-7. Epub 2007 Feb 8.
Yun HM, Kim S, Kim HJ, Kostenis E, Kim JI, Seong JY, Baik JH, Rhim H. The novel cellular mechanism of human 5-HT6 receptor through an interaction with Fyn J Biol Chem. 2007 Feb 23;282(8):5496-505. Epub 2006 Dec 22.
Park JH, Choi JK, Lee E, Lee JK, Rhim H, Seo SH, Kim Y, Doddareddy MR, Pae AN, Kang J, Roh EJ. Lead discovery and optimization of T-type calcium channel blockers Bioorg Med Chem. 2007 Feb 1;15(3):1409-19. Epub 2006 Nov 10.
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2006
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Takayasu S, Sakurai T, Iwasaki S, Teranishi H, Yamanaka A, Williams SC, Iguchi H, Kawasawa YI, Ikeda Y, Sakakibara I, Ohno K, Ioka RX, Murakami S, Dohmae N, Xie J, Suda T, Motoike T, Ohuchi T, Yanagisawa M, Sakai J. A neuropeptide ligand of the G protein-coupled receptor GPR103 regulates feeding, behavioral arousal, and blood pressure in mice Proc Natl Acad Sci U S A. 2006 May 9;103(19):7438-43. Epub 2006 Apr 28.
Taniguchi Y, Tonai-Kachi H, Shinjo K. Zaprinast, a well-known cyclic guanosine monophosphate-specific phosphodiesterase inhibitor, is an agonist for GPR35 FEBS Lett. 2006 Sep 18;580(21):5003-8. Epub 2006 Aug 17.
Akasofu S, Kimura M, Kosasa T, Ogura H, Sawada K. Protective effect of donepezil in primary-cultured rat cortical neurons exposed to N-methyl-d-aspartate (NMDA) toxicity Eur J Pharmacol. 2006 Jan 20;530(3):215-22.
Tang Y, Zhou L, Gunnet JW, Wines PG, Cryan EV, Demarest KT. Enhancement of arachidonic acid signaling pathway by nicotinic acid receptor HM74A Biochem Biophys Res Commun. 2006 Jun 23;345(1):29-37. Epub 2006 Apr 25.
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2005
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Nakae K, Hayashi F, Hayashi M, Yamamoto N, Iino T, Yoshikawa S, Gupta J. Functional role of prostacyclin receptor in rat dorsal root ganglion neurons Neurosci Lett. 2005 Nov 18;388(3):132-7.
Rodriguez AL, Nong Y, Sekaran NK, Alagille D, Tamagnan GD, Conn PJ. A close structural analog of 2-methyl-6-(phenylethynyl)-pyridine acts as a neutral allosteric site ligand on metabotropic glutamate receptor subtype 5 and blocks the effects of multiple allosteric modulators Mol Pharmacol. 2005 Dec;68(6):1793-802. Epub 2005 Sep 9.
Qiao SW, Piper J, Haraldsen G, Oynebråten I, Fleckenstein B, Molberg O, Khosla C, Sollid LM. Tissue transglutaminase-mediated formation and cleavage of histamine-gliadin complexes: biological effects and implications for celiac disease J Immunol. 2005 Feb 1;174(3):1657-63.
Iguchi H, Ikeda Y, Okamura M, Tanaka T, Urashima Y, Ohguchi H, Takayasu S, Kojima N, Iwasaki S, Ohashi R, Jiang S, Hasegawa G, Ioka RX, Magoori K, Sumi K, Maejima T, Uchida A, Naito M, Osborne TF, Yanagisawa M, Yamamoto TT, Kodama T, Sakai J. SOX6 attenuates glucose-stimulated insulin secretion by repressing PDX1 transcriptional activity and is down-regulated in hyperinsulinemic obese mice J Biol Chem. 2005 Nov 11;280(45):37669-80. Epub 2005 Sep 7.
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2004
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Inbe H, Watanabe S, Miyawaki M, Tanabe E, Encinas JA. Identification and characterization of a cell-surface receptor, P2Y15, for AMP and adenosine J Biol Chem. 2004 May 7;279(19):19790-9. Epub 2004 Mar 4.
Suga H, Takeda S, Haga T, Okamura M, Takao K, Tatemoto K. Stimulation of increases in intracellular calcium and prostaglandin E2 generation in Chinese hamster ovary cells expressing receptor-Galpha16 fusion proteins J Biochem. 2004 May;135(5):605-13.
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2003
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Le Poul E, Loison C, Struyf S, Springael JY, Lannoy V, Decobecq ME, Brezillon S, Dupriez V, Vassart G, Van Damme J, Parmentier M, Detheux M. Functional characterization of human receptors for short chain fatty acids and their role in polymorphonuclear cell activation J Biol Chem. 2003 Jul 11;278(28):25481-9. Epub 2003 Apr 23.
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2002
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Le Poul E, Hisada S, Mizuguchi Y, Dupriez VJ, Burgeon E, Detheux M. Adaptation of aequorin functional assay to high throughput screening J Biomol Screen. 2002 Feb;7(1):57-65.
Sumichika H, Sakata K, Sato N, Takeshita S, Ishibuchi S, Nakamura M, Kamahori T, Ehara S, Itoh K, Ohtsuka T, Ohbora T, Mishina T, Komatsu H, Naka Y. Identification of a potent and orally active non-peptide C5a receptor antagonist J Biol Chem. 2002 Dec 20;277(51):49403-7. Epub 2002 Oct 15.
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2001
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Kawamoto T, Kimura H, Kusumoto K, Fukumoto S, Shiraishi M, Watanabe T, Sawada H. Potent and selective inhibition of the human Na+/H+ exchanger isoform NHE1 by a novel aminoguanidine derivative T-162559 Eur J Pharmacol. 2001 May 18;420(1):1-8.
Maeda K, Yoshimura K, Shibayama S, Habashita H, Tada H, Sagawa K, Miyakawa T, Aoki M, Fukushima D, Mitsuya H. Novel low molecular weight spirodiketopiperazine derivatives potently inhibit R5 HIV-1 infection through their antagonistic effects on CCR5 J Biol Chem. 2001 Sep 14;276(37):35194-200. Epub 2001 Jul 13.
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